Ribociclib is a medication used in the treatment of certain types of cancer. It belongs to a class of drugs known as cyclin-dependent kinase (CDK) inhibitors. CDKs are enzymes involved in regulating the cell cycle, and inhibiting them can help slow down the growth and division of cancer cells.
Ribociclib is specifically indicated for the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. It is typically used in combination with an aromatase inhibitor as initial endocrine-based therapy in postmenopausal women, or in combination with fulvestrant in postmenopausal women or men.
The drug works by specifically inhibiting CDK4 and CDK6, which are proteins involved in promoting cell cycle progression. By inhibiting these proteins, ribociclib helps to halt the cell cycle at the G1 phase, preventing cancer cells from proliferating.
Ribociclib (Kisqali) Uses:
- Advanced or metastatic breast cancer:
- Ribociclib is used in pre/ peri or postmenopausal women as initial endocrine-based therapy for the management of (HR)-hormone receptor-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced or metastatic breast cancer (along with an aromatase inhibitor).
- In postmenopausal women, it is used in combination with fulvestrant as initial endocrine-based therapy or following disease progression on endocrine therapy in the management of HR-positive, HER2-negative advanced, or metastatic breast cancer.
Ribociclib (Kisqali) Dose in Adults
Note:
- If ribociclib is being used in combination with an aromatase inhibitor or fulvestrant for pre- or perimenopausal women, it's important to also give them a medication called a luteinizing hormone-releasing hormone (LHRH) agonist. This additional medication helps to block the production of certain hormones in the body, which is important for the effectiveness of the treatment.
Ribociclib (Kisqali) Dose in the treatment of advanced or metastatic Breast cancer:
- In the treatment of advanced or metastatic breast cancer in females who are hormone receptor-positive and HER2-negative, the recommended dose of ribociclib is 600 mg taken orally once daily for 21 days.
- This is followed by a 7-day rest period, completing a 28-day treatment cycle.
- Ribociclib is typically used in combination with either an aromatase inhibitor or fulvestrant.
- The treatment should be continued until there is disease progression or unacceptable side effects occur.
Missed doses:
- If a dose of ribociclib is missed or if vomiting occurs, it is advised not to take an additional dose on the same day. Instead, the regular dosing schedule should be resumed with the next scheduled dose.
Dosage adjustment for concomitant strong CYP3A inhibitors:
- When ribociclib is used concomitantly with strong CYP3A inhibitors, it is generally recommended to avoid their concurrent use if possible. It is advised to consider alternative medications with less potential for CYP3A inhibition in such cases.
- However, if coadministration with a strong CYP3A inhibitor cannot be avoided, the ribociclib dose should be reduced to 400 mg taken orally once daily.
- When the strong CYP3A inhibitor is discontinued, the ribociclib dose should be increased back to the dose that was used prior to initiating the strong CYP3A inhibitor. This increase should occur after at least 5 half-lives of the strong CYP3A4 inhibitor have passed.
Use in Children:
Not indicated.
Ribociclib (Kisqali) Pregnancy Risk Category: N
- Ribociclib can potentially harm a developing fetus if used during pregnancy, based on its effects and studies conducted on animals.
- Therefore, women who are capable of becoming pregnant should undergo a pregnancy test before starting ribociclib treatment.
- It is important to use effective contraception methods during treatment with ribociclib and for at least three weeks after the last dose to prevent pregnancy and ensure the safety of both the mother and potential baby.
Ribociclib use during breastfeeding:
- The presence of ribociclib in breast milk is not known, and therefore, it is uncertain if it can pass to the infant through breastfeeding.
- To prioritize the safety of the breastfeeding infant, the manufacturer advises against breastfeeding while undergoing ribociclib therapy or for a minimum of three weeks after the last dose of ribociclib.
Ribociclib (Kisqali) Dose in Renal Disease:
- For patients with an estimated glomerular filtration rate (eGFR) of 30 to less than 90 mL/minute/1.73 m², no dosage adjustment is necessary when taking ribociclib.
- For patients with an eGFR of 15 to less than 30 mL/minute/1.73 m², it is recommended to reduce the initial dose of ribociclib to 200 mg once daily. This recommendation is based on a study conducted in individuals without cancer. It's important to note that ribociclib has not been specifically studied in breast cancer patients with severe renal impairment.
- For patients with end-stage renal disease (eGFR less than 15 mL/minute/1.73 m²), the manufacturer's labeling does not provide specific dosage adjustments for ribociclib. Additionally, ribociclib has not been studied in breast cancer patients with severe renal impairment. It is advisable to consult with a healthcare professional to determine the most appropriate course of action for patients with severe renal impairment.
Ribociclib (Kisqali) Dose in Liver Disease:
Hepatic Impairment at Baseline:
|
Hepatic Impairment |
Dosage Adjustment |
|
Mild (Child-Pugh class A) |
No adjustment necessary |
|
Moderate or severe (Child-Pugh class B or C) |
Reduce initial dose to 400 mg once daily |
Hepatobiliary Toxicity during Treatment:
|
Grade of Elevations |
Dosage Adjustment |
|
Grade 1 (ALT and/or AST elevated >1 to 3 times ULN) |
No adjustment necessary |
|
Grade 2 (ALT and/or AST elevated >3 to 5 times ULN) |
If baseline was below grade 2, interrupt treatment until recovery and then resume ribociclib at the same dose level. For recurrent grade 2 elevations, interrupt treatment until recovery and then resume ribociclib at the next lower dose level. If baseline was at grade 2, no adjustment necessary. |
|
Grade 3 (ALT and/or AST elevated >5 to 20 times ULN) |
Interrupt treatment until recovery to baseline or lower, and then resume ribociclib at the next lower dose level. For recurrent grade 3 elevations, discontinue ribociclib. |
|
Grade 4 (ALT and/or AST elevated >20 times ULN) |
Discontinue ribociclib. |
Combined ALT and/or AST Elevations >3 times ULN with Total Bilirubin Increase >2 times ULN (in the absence of cholestasis), regardless of baseline grade:
- Discontinue ribociclib.
Common Side Effects of Ribociclib (Kisqali):
- Central Nervous System:
- Headache
- Insomnia
- Fatigue
- Dizziness
- Cardiovascular:
- Peripheral edema
- Renal:
- Increased Serum Creatinine
- Respiratory:
- Cough
- Dyspnea
- Gastrointestinal:
- Vomiting
- Constipation
- Decreased Appetite
- Nausea
- Abdominal Pain
- Stomatitis
- Diarrhoea
- Dermatologic:
- Pruritis
- Skin Rash
- Alopecia
- Endocrine & Metabolic:
- Decreased Serum Albumin
- Decreased Serum Potassium
- Increased Gamma-Glutamyl Transferase
- Decreased Serum Glucose
- Hematologic & Oncologic:
- Decreased Hemoglobin
- Leukemia
- Lymphocytopenia
- Anemia
- Abnormal Phosphorus Levels
- Neutropenia
- Genitourinary:
- Urinary Tract Infection
- Hepatic:
- Increased Serum Aspartate Aminotransferase
- Increased Serum Alanine Aminotransferase
- Abnormal Hepatic Function Tests
- Infection:
- Infection
- Neuromuscular & Skeletal:
- Arthralgia
- Back Pain
- Asthenia
- Miscellaneous:
- Fever
Less Common Side Effects of Ribociclib (Kisqali):
- Central Nervous System:
- Vertigo
- Cardiovascular:
- Prolonged Q-T Interval On ECG
- Syncope
- Dermatologic:
- Vitiligo
- Xeroderma
- Erythema
- Endocrine & Metabolic:
- Hypocalcemia
- Gastrointestinal:
- Dyspepsia
- Xerostomia
- Dysgeusia
- Hematologic & Oncologic:
- Febrile Neutropenia
- Thrombocytopenia
- Hepatic:
- Increased Serum Bilirubin
- Neuromuscular & Skeletal:
- Limb Pain
- Ophthalmic:
- Increased lacrimation
- Dry Eye Syndrome
- Respiratory:
- Oropharyngeal Pain
Contraindications to Ribociclib (Kisqali):
In the manufacturer's labeling, there are no contraindications listed for ribociclib.
In the Canadian labeling, there are additional contraindications not mentioned in the US labeling.
These contraindications include:
- Hypersensitivity: Ribociclib should not be used in individuals who have a known hypersensitivity to ribociclib or any component of the formulation.
- Untreated Congenital Long QT Syndrome: Ribociclib is contraindicated in individuals with untreated congenital long QT syndrome, which is a condition characterized by abnormal heart rhythms.
- Fridericia-corrected QT Interval (QTcF) ≥450 msec at baseline and patients at significant risk of developing QTc prolongation: Ribociclib should not be used in individuals with a baseline QTcF interval of 450 milliseconds or more, as well as those at significant risk of developing QTc prolongation, a condition that can increase the risk of abnormal heart rhythms.
Warnings and Precautions
Bone marrow suppression:
- Bone marrow suppression is a common side effect of ribociclib, and it often leads to a decrease in the number of neutrophils (a type of white blood cell).
- Grades 3 and 4 neutropenia, which indicate more severe reductions in neutrophil counts, can occur.
- Grade 2 or higher neutropenia typically starts around 16 days after starting treatment.
- It takes about 12 days, on average, for grade 3 or higher neutropenia to resolve and return to normal levels or less severe toxicity.
- Neutropenic fever, which is a fever associated with low neutrophil levels, has been observed.
- Regular blood count monitoring is important, with baseline measurements and subsequent checks every two weeks for the first two treatment cycles, and then at the beginning of each subsequent four cycles or as needed based on clinical judgment.
- Neutropenia may require treatment interruption, dose reduction, or even discontinuation of ribociclib depending on its severity.
- Other blood-related side effects such as anemia (low red blood cell count), thrombocytopenia (low platelet count), and lymphopenia (low lymphocyte count) have also been observed.
Hepatobiliary toxicity:
- Hepatobiliary toxicity is a known side effect of ribociclib, which can cause elevations in liver enzymes such as ALT and/or AST.
- Grade 3 or 4 events, indicating more severe elevations, have been observed.
- The onset of grade 3 or higher elevations typically occurs around 85 days after starting treatment, and it takes about 22 days, on average, for these elevations to improve to grade 2 or lower levels.
- In rare cases, simultaneous elevation of ALT or AST greater than three times the upper limit of normal (ULN) and total bilirubin greater than two times the ULN, without cholestasis (a condition affecting bile flow), has been reported.
- These cases resolved after discontinuing ribociclib.
- It is important to regularly monitor liver function tests, with baseline measurements and subsequent checks every two weeks for the first two treatment cycles, and then at the beginning of each subsequent four cycles or as needed based on clinical judgment.
- Depending on the severity of hepatobiliary toxicity, treatment interruption, dose reduction, or discontinuation of ribociclib may be necessary.
QT prolongation:
- Ribociclib can cause QT prolongation, which is a delay in the electrical activity of the heart.
- This effect is concentration-dependent, meaning it becomes more significant with higher drug levels in the body.
- At the recommended daily dose of 600 mg, ribociclib has been associated with an average increase in the QT interval of more than 20 milliseconds.
- Prolongation of the QTcF interval, a corrected measurement of the QT interval, exceeding 500 milliseconds has been observed, as well as increases of more than 60 milliseconds from baseline.
- These QT interval changes typically occur within the first four weeks of starting ribociclib treatment and can be reversed by temporarily interrupting treatment.
- While cases of torsades de pointes (a specific type of life-threatening arrhythmia) have not been reported, some patients have experienced fainting episodes (syncope).
- There has been one reported case of sudden death in a patient with low potassium levels and moderate QT prolongation.
- In a clinical trial, an increase of more than 60 milliseconds from baseline in the QTcF interval was seen more frequently in patients taking ribociclib with tamoxifen compared to those taking it with an aromatase inhibitor.
- Ribociclib is not recommended for use with tamoxifen.
- Before starting ribociclib, an electrocardiogram (ECG) should be evaluated, and treatment should only be initiated in patients with a QTcF interval less than 450 milliseconds.
- ECGs should be repeated on specific days of the treatment cycle and as clinically necessary.
- Regular monitoring of serum electrolytes, including potassium, magnesium, calcium, and phosphorous, is important, and any abnormalities should be corrected before starting ribociclib.
- If QT prolongation occurs, treatment interruption, dose reduction, or even discontinuation of ribociclib may be necessary.
- Ribociclib should be avoided in patients who have or are at significant risk for QT prolongation, including those with long QT syndrome, uncontrolled or significant cardiac disease (such as recent heart attack, heart failure, unstable angina, or slow heart rhythms), or electrolyte imbalances.
- It is also important to avoid concomitant use of ribociclib with medications known to prolong the QT interval and/or strong CYP3A inhibitors, as these can further increase the risk of QT prolongation.
Hepatic impairment
- For individuals with moderate or severe hepatic impairment, it is recommended to start ribociclib at a reduced initial dose.
- Hepatic impairment refers to a decreased functioning of the liver.
- In cases of moderate or severe impairment, the liver may not be able to process ribociclib as effectively as in individuals with normal liver function.
- To ensure the safety and appropriate use of ribociclib, the initial dose is adjusted to a lower amount in these patients.
Renal impairment:
- For individuals with severe renal impairment, it is recommended to start ribociclib at a reduced initial dose.
- Renal impairment refers to a decreased functioning of the kidneys, which are responsible for filtering waste products from the blood.
- In cases of severe impairment, the kidneys may not be able to effectively eliminate ribociclib from the body.
- To ensure the safe use of ribociclib in these individuals, the initial dose is adjusted to a lower amount.
- This adjustment helps to prevent the accumulation of ribociclib in the body, which can potentially lead to increased side effects or toxicity.
Ribociclib: Drug Interactions
|
Abemaciclib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Abemaciclib. |
|
AmLODIPine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of AmLODIPine. |
|
Apixaban |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Apixaban. |
|
ARIPiprazole |
|
|
Benzhydrocodone |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Benzhydrocodone. Specifically, the concentration of hydrocodone may be increased. |
|
Blonanserin |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Blonanserin. |
|
Bosentan |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Bosentan |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Bosentan. Management: Concomitant use of both a CYP2C9 inhibitor and a CYP3A inhibitor or a single agent that inhibits both enzymes with bosentan is likely to cause a large increase in serum concentrations of bosentan and is not recommended. See monograph for details. |
|
Brexpiprazole |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Brexpiprazole. Management: The brexpiprazole dose should be reduced to 25% of usual if used together with both a moderate CYP3A4 inhibitor and a strong or moderate CYP2D6 inhibitor, or if a moderate CYP3A4 inhibitor is used in a CYP2D6 poor metabolizer. |
|
Cannabidiol |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cannabidiol. |
|
Cannabis |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cannabis. More specifically, tetrahydrocannabinol and cannabidiol serum concentrations may be increased. |
|
Ceritinib |
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may enhance the QTcprolonging effect of Ceritinib. Ceritinib may enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of Ceritinib. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
Chloramphenicol (Ophthalmic) |
May enhance the adverse/toxic effect of Myelosuppressive Agents. |
|
Citalopram |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of Citalopram. |
|
Clofazimine |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Coccidioides immitis Skin Test |
Immunosuppressants may diminish the diagnostic effect of Coccidioides immitis Skin Test. |
|
Codeine |
CYP3A4 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Codeine. |
|
Crizotinib |
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may enhance the QTcprolonging effect of Crizotinib. QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of Crizotinib. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
CYP3A4 Inducers (Moderate) |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
CYP3A4 Inhibitors (Moderate) |
May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). |
|
CYP3A4 Substrates (High risk with Inhibitors) |
CYP3A4 Inhibitors (Moderate) may decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). Exceptions: Alitretinoin (Systemic); Praziquantel; Trabectedin; Vinorelbine. |
|
Deferasirox |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Denosumab |
May enhance the adverse/toxic effect of Immunosuppressants. Specifically, the risk for serious infections may be increased. |
|
Dronabinol |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dronabinol. |
|
Duvelisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Erdafitinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Erdafitinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Erythromycin (Systemic) |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
Estrogen Derivatives |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Estrogen Derivatives. |
|
Fluconazole |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
Fosnetupitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Haloperidol |
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may enhance the QTcprolonging effect of Haloperidol. Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
HYDROcodone |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of HYDROcodone. |
|
Ifosfamide |
CYP3A4 Inhibitors (Moderate) may decrease serum concentrations of the active metabolite(s) of Ifosfamide. |
|
Imatinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Imatinib. |
|
Larotrectinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Manidipine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Manidipine. |
|
Mesalamine |
May enhance the myelosuppressive effect of Myelosuppressive Agents. |
|
Mirodenafil |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Mirodenafil. |
|
Naldemedine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Naldemedine. |
|
Nalfurafine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Nalfurafine. |
|
Netupitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
NiMODipine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of NiMODipine. |
|
Ocrelizumab |
May enhance the immunosuppressive effect of Immunosuppressants. |
|
Ondansetron |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
OxyCODONE |
CYP3A4 Inhibitors (Moderate) may enhance the adverse/toxic effect of OxyCODONE. CYP3A4 Inhibitors (Moderate) may increase the serum concentration of OxyCODONE. Serum concentrations of the active metabolite Oxymorphone may also be increased. |
|
Palbociclib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Pentamidine (Systemic) |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
Pexidartinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pexidartinib. |
|
Pidotimod |
Immunosuppressants may diminish the therapeutic effect of Pidotimod. |
|
Promazine |
May enhance the myelosuppressive effect of Myelosuppressive Agents. |
|
QT-prolonging Antidepressants (Moderate Risk) |
May enhance the QTc-prolonging effect of QTprolonging Moderate CYP3A4 Inhibitors (Moderate Risk). Exceptions: Citalopram. |
|
QT-prolonging Antipsychotics (Moderate Risk) |
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may enhance the QTc-prolonging effect of QT-prolonging Antipsychotics (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Exceptions: Pimozide; QUEtiapine. |
|
QT-prolonging Class IC Antiarrhythmics (Moderate Risk) |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
QT-prolonging Kinase Inhibitors (Moderate Risk |
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may enhance the QTc-prolonging effect of QT-prolonging Kinase Inhibitors (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of QT-prolonging Kinase Inhibitors (Moderate Risk). Exceptions: Encorafenib; Entrectinib. |
|
QT-prolonging Miscellaneous Agents (Moderate Risk) |
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may enhance the QTc-prolonging effect of QT-prolonging Miscellaneous Agents (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of QT-prolonging Miscellaneous Agents (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Exceptions: Domperidone. |
|
QT-prolonging Quinolone Antibiotics (Moderate Risk) |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
QUEtiapine |
QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may enhance the QTcprolonging effect of QUEtiapine. QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of QUEtiapine. Management: Monitor for increased quetiapine toxicities including QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. |
|
Rupatadine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Rupatadine. |
|
Ruxolitinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ruxolitinib. |
|
Salmeterol |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Salmeterol. |
|
Sarilumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
SAXagliptin |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of SAXagliptin. |
|
Sildenafil |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Sildenafil. |
|
Silodosin |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Silodosin. |
|
Siltuximab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Siponimod |
Immunosuppressants may enhance the immunosuppressive effect of Siponimod. |
|
Tamsulosin |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Tamsulosin. |
|
Tertomotide |
Immunosuppressants may diminish the therapeutic effect of Tertomotide. |
|
Tetrahydrocannabinol |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Tetrahydrocannabinol. |
|
Ticagrelor |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ticagrelor. |
|
Tocilizumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Trabectedin |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Trabectedin. |
|
Trastuzumab |
May enhance the neutropenic effect of Immunosuppressants. |
|
Udenafil |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Udenafil. |
|
Vilazodone |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Vilazodone. |
|
Vindesine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Vindesine. |
|
Zuclopenthixol |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Zuclopenthixol. |
|
Risk Factor D (Consider therapy modification) |
|
|
Acalabrutinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Acalabrutinib. Management: Reduce acalabrutinib dose to 100 mg once daily with concurrent use of a moderate CYP3A4 inhibitor. Monitor patient closely for both acalabrutinib response and evidence of adverse effects with any concurrent use. |
|
Avanafil |
|
|
Baricitinib |
Immunosuppressants may enhance the immunosuppressive effect of Baricitinib. Management: Use of baricitinib in combination with potent immunosuppressants such as azathioprine or cyclosporine is not recommended. Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted. |
|
Brigatinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Brigatinib. Management: Avoid concurrent use of brigatinib with moderate CYP3A4 inhibitors when possible. If such a combination cannot be avoided, reduce the dose of brigatinib by approximately 40% (ie, from 180 mg to 120 mg, from 120 mg to 90 mg, or from 90 mg to 60 mg). |
|
Bromocriptine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Bromocriptine. Management: The bromocriptine dose should not exceed 1.6 mg daily with use of a moderate CYP3A4 inhibitor. The Cycloset brand specifically recommends this dose limitation, but other bromocriptine products do not make such specific recommendations. |
|
Budesonide (Topical) |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Budesonide (Topical). Management: Per US prescribing information, avoid this combination. Canadian product labeling does not recommend strict avoidance. If combined, monitor for excessive glucocorticoid effects as budesonide exposure may be increased. |
|
Cilostazol |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cilostazol. Management: Consider reducing the cilostazol dose to 50 mg twice daily in adult patients who are also receiving moderate inhibitors of CYP3A4. |
|
Colchicine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Colchicine. Management: Reduce colchicine dose as directed when using with a moderate CYP3A4 inhibitor, and increase monitoring for colchicine-related toxicity. See full monograph for details. Use extra caution in patients with impaired renal and/or hepatic function. |
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CYP3A4 Inhibitors (Strong) |
May increase the serum concentration of Ribociclib. Management: Avoid use of ribociclib with strong CYP3A4 inhibitors when possible; if combined use cannot be avoided, reduce ribociclib dose to 400 mg once daily. Exceptions are discussed in separate monographs. Exceptions: Voriconazole. |
|
Dabrafenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). |
|
Dapoxetine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dapoxetine. Management: The dose of dapoxetine should be limited to 30 mg per day when used together with a moderate inhibitor of CYP3A4. |
|
Deferiprone |
Myelosuppressive Agents may enhance the neutropenic effect of Deferiprone. Management: Avoid the concomitant use of deferiprone and myelosuppressive agents whenever possible. If this combination cannot be avoided, monitor the absolute neutrophil count more closely. |
|
Deflazacort |
CYP3A4 Inhibitors (Moderate) may increase serum concentrations of the active metabolite(s) of Deflazacort. Management: Administer one third of the recommended deflazacort dose when used together with a strong or moderate CYP3A4 inhibitor. |
|
DOXOrubicin (Conventional) |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of DOXOrubicin (Conventional). Management: Seek alternatives to moderate CYP3A4 inhibitors in patients treated with doxorubicin whenever possible. One U.S. manufacturer (Pfizer Inc.) recommends that these combinations be avoided. |
|
Echinacea |
May diminish the therapeutic effect of Immunosuppressants. |
|
Eletriptan |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Eletriptan. Management: The use of eletriptan within 72 hours of a moderate CYP3A4 inhibitor should be avoided. |
|
Eliglustat |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Eliglustat. Management: Use should be avoided under some circumstances. See full drug interaction monograph for details. |
|
Encorafenib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Encorafenib. Management: Avoid concomitant use of encorafenib and moderate CYP3A4 inhibitors whenever possible. If concomitant administration is unavoidable, decrease the encorafenib dose prior to initiation of the CYP3A4 inhibitor. See full monograph for details. |
|
Encorafenib |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of Encorafenib. Management: Avoid using moderate CYP3A4 inhibitors together with encorafenib if possible. If the combination must be used, reduce the encorafenib dose prior to initiation of the moderate CYP3A4 inhibitor and monitor QT interval. See full monograph for details. |
|
Eplerenone |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Eplerenone. Management: When used concomitantly with moderate inhibitors of CYP3A4, eplerenone dosing recommendations vary by indication and international labeling. See full drug interaction monograph for details. |
|
Everolimus |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Everolimus. Management: Everolimus dose reductions are required for most indications. See full monograph or prescribing information for specific dose adjustment and monitoring recommendations. |
|
FentaNYL |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of FentaNYL. Management: Monitor patients closely for several days following initiation of this combination, and adjust fentanyl dose as necessary. |
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Fingolimod |
Immunosuppressants may enhance the immunosuppressive effect of Fingolimod. Management: Avoid the concomitant use of fingolimod and other immunosuppressants when possible. If combined, monitor patients closely for additive immunosuppressant effects (eg, infections). |
|
GuanFACINE |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of GuanFACINE. Management: Reduce the guanfacine dose by 50% when initiating this combination. |
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Ibrutinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ibrutinib. Management: When treating B-cell malignancies, decrease ibrutinib to 280 mg daily when combined with moderate CYP3A4 inhibitors. When treating graft versus host disease, monitor patients closely and reduce the ibrutinib dose as needed based on adverse reactions. |
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Ivacaftor |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ivacaftor. Management: Ivacaftor dose reductions are required; consult full monograph content for specific age- and weight-based recommendations. No dose adjustment is needed when using ivacaftor/lumacaftor with a moderate CYP3A4 inhibitor. |
|
Leflunomide |
Immunosuppressants may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Management: Consider not using a leflunomide loading dose in patients receiving other immunosuppressants. Patients receiving both leflunomide and another immunosuppressant should be monitored for bone marrow suppression at least monthly. |
|
Lorlatinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. |
|
Lurasidone |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Lurasidone. Management: Lurasidone US labeling recommends reducing lurasidone dose by half with a moderate CYP3A4 inhibitor. Some non-US labeling recommends initiating lurasidone at 20 mg/day and limiting dose to 40 mg/day; avoid concurrent use of grapefruit products. |
|
Meperidine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Meperidine. Management: Consider reducing meperidine dose if concomitant use with moderate CYP3A4 inhibitors is required. Monitor for signs and symptoms of respiratory depression and sedation when these agents are combined. |
|
MiFEPRIStone |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. |
|
Nilotinib |
May enhance the QTc-prolonging effect of Ribociclib. Management: Consider alternatives to this combination. Patients with other risk factors (eg, older age, female sex, bradycardia, hypokalemia, hypomagnesemia, heart disease, and higher drug concentrations) are likely at greater risk for these toxicities. |
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Nivolumab |
Immunosuppressants may diminish the therapeutic effect of Nivolumab. |
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Olaparib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Olaparib. Management: Avoid use of moderate CYP3A4 inhibitors in patients being treated with olaparib, if possible. If such concurrent use cannot be avoided, the dose of olaparib should be reduced to 150 mg twice daily. |
|
QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk) |
Ribociclib may enhance the QTcprolonging effect of QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk). QT-prolonging Strong CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of Ribociclib. Management: Avoid concomitant use of ribociclib and strong CYP3A4 inhibitors that prolong the QTc interval whenever possible. If combined, decrease the ribociclib dose to 400 mg daily. Monitor for ribociclib toxicities including QTc prolongation and arrhythmias. |
|
Ranolazine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ranolazine. Management: Limit the ranolazine adult dose to a maximum of 500 mg twice daily in patients concurrently receiving moderate CYP3A4 inhibitors (e.g., diltiazem, verapamil, erythromycin, etc.). |
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Roflumilast |
May enhance the immunosuppressive effect of Immunosuppressants. |
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Sipuleucel-T |
Immunosuppressants may diminish the therapeutic effect of Sipuleucel-T. Management: Evaluate patients to see if it is medically appropriate to reduce or discontinue therapy with immunosuppressants prior to initiating sipuleucel-T therapy. |
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Sirolimus |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Sirolimus. Management: Monitor for increased serum concentrations of sirolimus if combined with a moderate CYP3A4 inhibitor. Lower initial sirolimus doses or sirolimus dose reductions will likely be required. |
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Sonidegib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Sonidegib. Management: Avoid concomitant use of sonidegib and moderate CYP3A4 inhibitors when possible. When concomitant use cannot be avoided, limit CYP3A4 inhibitor use to less than 14 days and monitor for sonidegib toxicity (particularly musculoskeletal adverse reactions). |
|
Stiripentol |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. |
|
Suvorexant |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Suvorexant. Management: The recommended dose of suvorexant is 5 mg daily in patients receiving a moderate CYP3A4 inhibitor. The dose can be increased to 10 mg daily (maximum dose) if necessary for efficacy. |
|
Tamoxifen |
Ribociclib may increase the serum concentration of Tamoxifen. Management: Concurrent use of ribociclib with tamoxifen is not indicated. Use of this combination may increase the effects and toxicities of tamoxifen. |
|
Tezacaftor |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Tezacaftor. Management: When combined with moderate CYP3A4 inhibitors, tezacaftor/ivacaftor should be given in the morning, every other day. Ivacaftor alone should be given in the morning, every other day on alternate days from tezacaftor/ivacaftor. |
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Tofacitinib |
Immunosuppressants may enhance the immunosuppressive effect of Tofacitinib. Management: Concurrent use with antirheumatic doses of methotrexate or nonbiologic disease modifying antirheumatic drugs (DMARDs) is permitted, and this warning seems particularly focused on more potent immunosuppressants. |
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Tolvaptan |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Tolvaptan. Management: Jynarque dose requires adjustment when used with a moderate CYP3A4 inhibitor. See labeling or full interaction monograph for specific recommendations. Use of Samsca with moderate CYP3A4 ihibitors should generally be avoided. |
|
Vaccines (Inactivated) |
Immunosuppressants may diminish the therapeutic effect of Vaccines (Inactivated). Management: Vaccine efficacy may be reduced. Complete all age-appropriate vaccinations at least 2 weeks prior to starting an immunosuppressant. If vaccinated during immunosuppressant therapy, revaccinate at least 3 months after immunosuppressant discontinuation. |
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Venetoclax |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Venetoclax. Management: Reduce the venetoclax dose by at least 50% in patients requiring these combinations. |
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Zopiclone |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Zopiclone. Management: The starting adult dose of zopiclone should not exceed 3.75 mg if combined with a moderate CYP3A4 inhibitor. Monitor patients for signs and symptoms of zopiclone toxicity if these agents are combined. |
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Risk Factor X (Avoid combination) |
|
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Aprepitant |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Aprepitant. |
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Asunaprevir |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Asunaprevir. |
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BCG (Intravesical) |
Immunosuppressants may diminish the therapeutic effect of BCG (Intravesical). |
|
BCG (Intravesical) |
Myelosuppressive Agents may diminish the therapeutic effect of BCG (Intravesical). |
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Bosutinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Bosutinib. |
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Budesonide (Systemic) |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Budesonide (Systemic). |
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Cladribine |
May enhance the immunosuppressive effect of Immunosuppressants. |
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Cladribine |
May enhance the myelosuppressive effect of Myelosuppressive Agents. |
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Cobimetinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Cobimetinib. Management: Avoid the concomitant use of cobimetinib and moderate CYP3A4 inhibitors. If concurrent short term (14 days or less) use cannot be avoided, reduce the cobimetinib dose to 20 mg daily. |
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Conivaptan |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
CYP3A4 Inducers (Strong) |
May decrease the serum concentration of Ribociclib. |
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Dipyrone |
May enhance the adverse/toxic effect of Myelosuppressive Agents. Specifically, the risk for agranulocytosis and pancytopenia may be increased |
|
Domperidone |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of Domperidone. |
|
Entrectinib |
May enhance the QTc-prolonging effect of QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk). QT-prolonging Moderate CYP3A4 Inhibitors (Moderate Risk) may increase the serum concentration of Entrectinib. |
|
Flibanserin |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Flibanserin. |
|
Fosaprepitant |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Fosaprepitant. |
|
Fusidic Acid (Systemic) |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Grapefruit Juice |
May increase the serum concentration of Ribociclib. |
|
Idelalisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Ivabradine |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ivabradine. |
|
Lefamulin |
May enhance the QTc-prolonging effect of QT-prolonging CYP3A4 Substrates. Management: Do not use lefamulin tablets with QT-prolonging CYP3A4 substrates. Lefamulin prescribing information lists this combination as contraindicated. |
|
Lomitapide |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Lomitapide. |
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Naloxegol |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Naloxegol. |
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Natalizumab |
Immunosuppressants may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. |
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Neratinib |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Neratinib. |
|
Pimecrolimus |
May enhance the adverse/toxic effect of Immunosuppressants. |
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Pimozide |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Pimozide. |
|
Pimozide |
May enhance the QTc-prolonging effect of QT-prolonging Agents (Moderate Risk). |
|
Pomegranate |
May increase the serum concentration of Ribociclib. |
|
Posaconazole |
May increase the serum concentration of QT-prolonging CYP3A4 Substrates. Such increases may lead to a greater risk for proarrhythmic effects and other similar toxicities. |
|
QT-prolonging Agents (Highest Risk) |
May enhance the QTc-prolonging effect of Ribociclib. |
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Simeprevir |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Simeprevir. |
|
St John's Wort |
May decrease the serum concentration of Ribociclib. |
|
Tacrolimus (Topical) |
May enhance the adverse/toxic effect of Immunosuppressants. |
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Ulipristal |
CYP3A4 Inhibitors (Moderate) may increase the serum concentration of Ulipristal. Management: This is specific for when ulipristal is being used for signs/symptoms of uterine fibroids (Canadian indication). When ulipristal is used as an emergency contraceptive, patients receiving this combination should be monitored for ulipristal toxicity. |
|
Vaccines (Live) |
Immunosuppressants may enhance the adverse/toxic effect of Vaccines (Live). Immunosuppressants may diminish the therapeutic effect of Vaccines (Live). Management: Avoid use of live organism vaccines with immunosuppressants; live-attenuated vaccines should not be given for at least 3 months after immunosuppressants. |
Monitoring Parameters:
Complete blood count:
- Baseline measurement
- Every 2 weeks for the first 2 cycles
- At the beginning of each subsequent 4 cycles
- As clinically necessary
Liver function tests:
- Baseline measurement
- Every 2 weeks for the first 2 cycles
- At the beginning of each subsequent 4 cycles
- As clinically necessary
Serum electrolytes:
- Including potassium, magnesium, calcium, and phosphorous
- Prior to treatment initiation
- At the beginning of each of the first 6 cycles
- As clinically indicated
Pregnancy test:
- Prior to treatment in females of reproductive potential
ECG (Electrocardiogram):
- Prior to treatment initiation
- Repeat on day 14 of cycle 1
- At the beginning of cycle 2
- As clinically indicated
Monitor adherence to the prescribed treatment regimen.
Regular monitoring of these parameters helps ensure the safety and effectiveness of ribociclib treatment.
How to administer Ribociclib (Kisqali)?
- Food: Ribociclib can be taken with or without food. There is no specific requirement regarding food intake.
- Timing: It is recommended to take ribociclib at approximately the same time each day, preferably in the morning. This helps establish a consistent dosing schedule and can assist with remembering to take the medication regularly.
- Swallowing: The tablets should be swallowed whole. They should not be crushed, chewed, or split. It is important not to ingest broken or cracked tablets, as this can affect the proper delivery of the medication.
Following these administration instructions ensures that ribociclib is taken correctly and optimizes its absorption and effectiveness in the body.
Mechanism of action of Ribociclib (Kisqali):
- Ribociclib is a type of medication that works by blocking certain proteins in the cells called cyclin-dependent kinases (CDK) 4 and 6.
- By doing so, it stops the cells from progressing through the cell cycle and gets them stuck in a specific phase called G1.
- This helps to slow down or stop the growth of cancer cells.
- When ribociclib is used together with an aromatase inhibitor or fulvestrant, it has shown to be more effective in inhibiting tumor growth compared to using each drug alone.
- This combination therapy has been particularly effective in treating estrogen receptor positive breast cancer.
Distribution:
- Ribociclib has a large volume of distribution (V/F) of approximately 1,090 liters, which indicates that it spreads widely throughout the body.
Protein Binding:
- It is highly bound to proteins in the blood, with an approximate binding capacity of 70%.
- This means that a significant portion of ribociclib attaches to proteins in the bloodstream.
Metabolism:
- Ribociclib is extensively metabolized in the liver, mainly through the action of an enzyme called CYP3A4.
- It undergoes oxidation, resulting in the formation of metabolites known as M13, M4, and M1.
- However, the main clinical activity of ribociclib is primarily attributed to the original (parent) drug.
Half-life:
- The elimination half-life of ribociclib in the body's circulation is approximately 30 to 55 hours.
- This means it takes this amount of time for half of the drug to be cleared from the body.
Time to Peak:
- After oral administration, ribociclib reaches its peak concentration in the bloodstream within 1 to 4 hours.
Excretion:
- Ribociclib and its metabolites are mainly excreted through feces (69%), with approximately 17% of the drug remaining unchanged and 14% as the M1 metabolite.
- A smaller portion is eliminated through urine (23%), with around 12% of the parent drug and 4% as the M1 metabolite.
- Other metabolites account for less than 3% of excretion.
International Brand Names of Ribociclib:
- Kisqali (200 MG Dose)
- Kisqali (400 MG Dose)
- Kisqali (600 MG Dose)
- Kryxana
Ribociclib Brand Names in Pakistan:
Kisqali (200 MG Dose)
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