Ribociclib

What is Ribociclib

Ribociclib is an oral, selective inhibitor of cyclin-dependent kinases (CDKs) 4 and 6, which are both involved in tumor cell progression during phase G1 to phase S in the cell cycle.

By inhibiting CDK 4 and 6, ribociclib prevents the deactivation of the tumor suppressor protein known as retinoblastoma susceptibility gene protein, and interferes with tumor cell progression.

Ribociclib is FDA-approved for the initial endocrine-based treatment of hormone receptor (HR)-positive, HER2-negative advanced or metastatic breast cancer in combination with an aromatase inhibitor in pre/peri/postmenopausal women, and in combination with fulvestrant for the treatment of postmenopausal women with HR-positive, HER2-negative advanced or metastatic breast cancer, either as initial endocrine based therapy or following disease progression on endocrine therapy.

Brand Name

KISQALI

Indications & Dosage

  • breast cancer

For the treatment of breast cancer

for the first-line treatment of HR-positive, HER2-negative advanced or metastatic breast cancer as initial endocrine-based therapy, in combination with an aromatase inhibitor

Side Effects

  1. abdominal pain
  2. acute respiratory distress syndrome (ARDS)
  3. alopecia
  4. anemia
  5. anorexia
  6. arthralgia
  7. asthenia
  8. back pain
  9. constipation
  10. cough
  11. diarrhea
  12. dizziness
  13. dysgeusia
  14. dyspnea
  15. elevated liver enzymes
  16. erythema
  17. fatigue
  18. fever
  19. headache
  20. hyperbilirubinemia
  21. hypocalcemia
  22. hypoglycemia
  23. hypokalemia
  24. hypophosphatemia
  25. infection
  26. insomnia
  27. interstitial lung disease
  28. lacrimation
  29. leukopenia
  30. lymphopenia
  31. nausea
  32. neutropenia
  33. peripheral edema
  34. pneumonitis
  35. pruritus
  36. pulmonary fibrosis
  37. QT prolongation
  38. rash
  39. renal failure (unspecified)
  40. stomatitis
  41. syncope
  42. thrombocytopenia
  43. vertigo
  44. vomiting
  45. xerophthalmia
  46. xerosis
  47. xerostomia

Monitoring Parameters

  • CBC with differential
  • ECG
  • LFTs
  • pregnancy testing
  • serum electrolytes

Contraindications

  • alcoholism
  • bone marrow suppression
  • bradycardia
  • breast-feeding
  • cardiac arrhythmias
  • cardiac disease
  • chronic lung disease (CLD)
  • contraception requirements
  • coronary artery disease
  • diabetes mellitus
  • electrolyte imbalance
  • females
  • geriatric
  • heart failure
  • hepatic disease
  • hepatotoxicity
  • hypertension
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • infertility
  • long QT syndrome
  • malnutrition
  • myocardial infarction
  • neutropenia
  • pneumonitis
  • pregnancy
  • pregnancy testing
  • QT prolongation
  • reproductive risk
  • thyroid disease

Interactions

  • Abacavir; Dolutegravir; Lamivudine
  • Abemaciclib
  • Acalabrutinib
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
  • Acetaminophen; Codeine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Aclidinium; Formoterol
  • Ado-Trastuzumab emtansine
  • Albuterol
  • Albuterol; Ipratropium
  • Alfentanil
  • Alfuzosin
  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Almotriptan
  • Alosetron
  • Alprazolam
  • Amiodarone
  • Amitriptyline
  • Amitriptyline; Chlordiazepoxide
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Anagrelide
  • Apalutamide
  • Apomorphine
  • Aprepitant, Fosaprepitant
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  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Carisoprodol; Codeine
  • Aspirin, ASA; Oxycodone
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  • Bupivacaine; Lidocaine
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  • Chlorpheniramine; Dihydrocodeine; Phenylephrine
  • Chlorpheniramine; Dihydrocodeine; Pseudoephedrine
  • Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
  • Chlorpheniramine; Hydrocodone
  • Chlorpheniramine; Hydrocodone; Phenylephrine
  • Chlorpheniramine; Hydrocodone; Pseudoephedrine
  • Chlorpromazine
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  • Ethinyl Estradiol; Ethynodiol Diacetate
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  • Goserelin
  • Granisetron
  • grapefruit juice
  • Guaifenesin; Hydrocodone
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  • Guanfacine
  • Halogenated Anesthetics
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  • Halothane
  • Histrelin
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  • Hydrocodone; Potassium Guaiacolsulfonate
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  • Ziprasidone
  • Zolpidem
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