Kisqali

In combination w/ an aromatase inhibitor for the adjuvant treatment of adults w/ hormone receptor (HR) +ve, human epidermal growth factor receptor 2 (HER2) -ve stage II & III early breast cancer at high risk of recurrence. Treatment of women w/ HR +ve, HER2 -ve advanced or metastatic breast cancer in combination w/ an aromatase inhibitor as initial endocrine-based therapy, or fulvestrant as initial endocrine-based therapy or following disease progression on endocrine therapy.

Early breast cancer 400 mg once daily for 21 consecutive days followed by 7 days off in 28-day treatment cycles. Patient w/ severe renal impairment Initially 200 mg once daily. Advanced or metastatic breast cancer 600 mg once daily for 21 consecutive days followed by 7 days off in 28-day treatment cycles. Patient w/ moderate or severe hepatic impairment Initially 400 mg once daily. Patient w/ severe renal impairment Initially 200 mg once daily.

May be taken with or without food: Swallow whole. Do not chew/crush/split. Do not ingest if broken/cracked/not intact.

Risk of severe, life-threatening, or fatal ILD &/or pneumonitis; severe cutaneous adverse reactions (SCARs), including SJS, TEN, & drug-induced hypersensitivity syndrome/DRESS; QT interval prolongation; drug-induced liver injury & increased transaminases; neutropenia. Monitor for pulmonary symptoms indicative of ILD/pneumonitis, & signs or symptoms of severe cutaneous reactions. Perform ECG prior to starting treatment, then repeat at approx day 14 of the 1st cycle, & as clinically indicated. Monitor serum electrolytes (including K, Ca, P, Mg) prior to treatment initiation at the beginning of the 1st 6 cycles, & as clinically indicated. Perform LFTs & CBC before initiating treatment, then monitor every 2 wk for the 1st 2 cycles, at the beginning of each subsequent 4 cycles, & as clinically indicated. Interrupt treatment in case of grade 2 ILD/pneumonitis; grade 3 cutaneous adverse reactions, including SCARs; QTcF >480-500 ms; AST &/or ALT >3-20x ULN from baseline w/o increase in total bilirubin >2x ULN; grade 3 or 4 neutropenia or grade 3 febrile neutropenia. Discontinue treatment in case of grade 3 or 4 ILD/pneumonitis; grade 4 cutaneous adverse reactions, including SCARs; QTcF >500 ms or >60 ms change from baseline & associated w/ torsades de pointes, polymorphic ventricular tachycardia, syncope, or signs/symptoms of serious arrhythmia; AST &/or ALT >20x ULN from baseline w/o increase in total bilirubin >2x ULN, or AST &/or ALT >3x ULN w/ increase in total bilirubin >2x ULN irrespective of baseline. Do not reintroduce treatment in patients who have experienced SCARs or other life-threatening cutaneous reactions during treatment. Avoid use in patients who are at significant risk of developing torsades de pointes. Initiate treatment only in patients w/ QTcF <450 ms. Avoid concomitant use w/ strong CYP3A inhibitors; strong CYP3A inducers; drugs known to prolong QT interval; tamoxifen. Can cause fetal harm when administered to a pregnant woman. Females of reproductive potential should use effective contraception during treatment & for at least 3 wk after the last dose. May impair fertility in males of reproductive potential. Do not breastfeed during treatment & for at least 3 wk after the last dose. Safety & efficacy in ped patients have not been established.

Early breast cancer: Decreased lymphocytes, decreased leukocytes, decreased neutrophils, decreased Hb, increased ALT, increased AST, infections, increased creatinine, decreased platelets, headache, nausea, fatigue. Advanced or metastatic breast cancer: Decreased leukocytes, decreased neutrophils, decreased Hb, decreased lymphocytes, increased AST, increased γ-glutamyl transferase, increased ALT, infections, nausea, increased creatinine, fatigue, decreased platelets, diarrhea, vomiting, headache, constipation, alopecia, cough, rash, back pain, decreased serum glucose.

Increased exposure w/ strong CYP3A inhibitors. Decreased exposure w/ strong CYP3A inducers. Increased exposure of sensitive CYP3A4 substrates. Avoid co-administration w/ drugs that have known potential to prolong QT interval eg, antiarrhythmic drugs & other drugs that are known to prolong QT interval.

Targeted Cancer Therapy

L01EF02 - ribociclib ; Belongs to the class of cyclin-dependent kinase (CDK) inhibitors. Used in the treatment of cancer.

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