Kryxana

Ribociclib

In combination w/ an aromatase inhibitor or fulvestrant for patients w/ hormone receptor (HR) +ve, human epidermal growth factor receptor 2 (HER2) -ve (locally) advanced or metastatic breast cancer. In combination w/ endocrine therapy & a luteinizing hormone releasing hormone (LHRH) agonist for pre- or peri-menopausal women.

600 mg once daily (as three 200 mg tab) for 21 consecutive days followed by 7 days off treatment resulting in a complete cycle of 28 days. Dose modification: 1st dose reduction: 400 mg/day (as two 200 mg tab). 2nd dose reduction: 200 mg/day. Co-administration w/ strong CYP3A4 inhibitor Reduce dose to 200 mg once daily. Severe renal impairment Initially 200 mg. Moderate (Child-Pugh class B) & severe (Child-Pugh class C) hepatic impairment Initially 400 mg.

May be taken with or without food: Take at the same time every day, preferably in the morning. Swallow whole, do not chew/crush/split.

Hypersensitivity.

Discontinue immediately & permanently if signs & symptoms suggestive of severe cutaneous reactions (eg, progressive widespread skin rash often w/ blisters or mucosal lesions) appear. Monitor patients for pulmonary symptoms indicative of interstitial lung disease/pneumonitis. Perform complete blood count & liver function tests before initiating therapy & monitor every 2 wk for the 1st 2 cycles, at the beginning of each of the subsequent 4 cycles, then as clinically indicated. Assess ECG prior to initiation of treatment & repeat at approx day 14 of the 1st cycle, at the beginning of the 2nd cycle, & then as clinically indicated; only initiate treatment in patients w/ QTcF interval values <450 ms. Monitor serum electrolytes (including K, Ca, P, & Mg) prior to initiation of treatment, at the beginning of the 1st 6 cycles, & then as clinically indicated; correct any abnormality before & during therapy. Avoid in patients who already have or at risk of developing QTc interval prolongation including those w/ long QT syndrome, uncontrolled or significant cardiac diseases (including recent MI, CHF, unstable angina & bradyarrhythmias), electrolyte abnormalities. Avoid in combination w/ medicinal products known to prolong QTc interval &/or strong CYP3A inhibitors. Combination w/ tamoxifen is not recommended. Women of reproductive potential should use effective contraception methods during treatment & for 21 days after stopping treatment. Pregnancy (may cause fetal harm). Avoid use during lactation (& for at least 21 days after the last dose).

Infections; neutropenia, leukopenia, anemia; decreased appetite; headache, dizziness; dyspnea, cough; back pain; nausea, diarrhea, vomiting, constipation, stomatitis, abdominal pain; alopecia, rash, pruritus; fatigue, peripheral edema, asthenia, pyrexia; abnormal liver function tests; decreased leukocyte, neutrophil, Hb, lymphocyte, & platelet count; increased ALT, AST, creatinine, γ-glutamyl transferase; decreased P, albumin, glucose serum. Lymphopenia, thrombocytopenia, febrile neutropenia; increased lacrimation, dry eye; hypocalcemia, hypokalemia, hypophosphatemia; vertigo; syncope; dysgeusia, dyspepsia; hepatotoxicity; erythema, dry skin, vitiligo; dry mouth, oropharyngeal pain; increased blood creatinine, prolonged ECG QT; decreased K, increased bilirubin.

Increased exposure w/ strong CYP3A inhibitors (eg, clarithromycin, indinavir, itraconazole, ketoconazole, lopinavir, ritonavir, nefazodone, nelfinavir, posaconazole, ritonavir, saquinavir, telaprevir, telithromycin, verapamil & voriconazole) & grapefruit or grapefruit juice. Decreased plasma exposure w/ strong CYP3A inducers eg, phenytoin, rifampin, carbamazepine & St. John's wort. Increased exposure of midazolam, alfentanil, cyclosporine, dihydroergotamine, ergotamine, everolimus, fentanyl, pimozide, quinidine, sirolimus, tacrolimus; caffeine; tamoxifen. Potential to prolong the QT interval w/ antiarrhythmics (eg, amiodarone, disopyramide, procainamide, quinidine, & sotalol), & other medicinal products (eg, chloroquine, halofantrine, clarithromycin, ciprofloxacin, levofloxacin, azithromycin, haloperidol, methadone, moxifloxacin, bepridil, pimozide & ondansetron IV).

Targeted Cancer Therapy

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

Rx