Leukemias, lymphomas, and other hematologic cancers:

Indications for TIBSOVO:

Newly-diagnosed acute myeloid leukemia (AML) with a susceptible isocitrate dehydrogenase-1 (IDH1) mutation as detected by an FDA-approved test in adults ≥75yrs old or have comorbidities that preclude use of intensive induction chemotherapy. Relapsed or refractory AML with a susceptible IDH1 mutation as detected by an FDA-approved test.

Adult:

Swallow whole. Take at same time each day. Avoid a high-fat meal. 500mg once daily until disease progression or unacceptable toxicity. Without disease progression or unacceptable toxicity: treat for a minimum of 6 months to allow time for response. If concomitant strong CYP3A4 inhibitor is unavoidable: reduce to 250mg once daily; when inhibitor is discontinued, resume at 500mg once daily (after at least 5 half-lives of the inhibitor). Monitoring and dose modifications for toxicities: see full labeling.

Children:

Not established.

Boxed Warning:

Differentiation syndrome.

Warnings/Precautions:

Risk of differentiation syndrome (may be fatal if not treated). If differentiation syndrome is suspected, initiate oral or IV corticosteroids and hemodynamic monitoring until resolution; interrupt dose if severe symptoms persist >48hrs after corticosteroid initiation. Assess blood counts/chemistries prior to initiation, at least weekly for the first month, once every other week for the second month, and once monthly thereafter. Monitor creatine phosphokinase weekly for the first month. Monitor ECG at least weekly for the first 3 weeks, then at least monthly thereafter. Congenital long QT syndrome, CHF, electrolyte abnormalities: monitor more frequently. Interrupt therapy if QTc >480–<500msec; interrupt and reduce dose if >500msec; permanently discontinue if QTc prolongation with life-threatening arrhythmias develop. Monitor for new motor and/or sensory neuropathy (eg, unilateral or bilateral weakness, sensory alterations, paresthesias, difficulty breathing); permanently discontinue if Guillain-Barré syndrome diagnosed. Severe renal or hepatic impairment. Hemodialysis. Pregnancy: may cause fetal harm. Nursing mothers: not recommended (during and for at least 1 month after final dose).

Pharmacologic Class:

Isocitrate dehydrogenase-1 (IDH1) inhibitor.

Interactions:

See Adults. May increase risk of QT prolongation when concomitant drugs known to prolong QTc interval (eg, antiarrhythmics, fluoroquinolones, triazole antifungals, 5-HT3 receptor antagonists) or with CYP3A4 inhibitors; avoid or use alternatives. Antagonized by strong CYP3A4 inducers; avoid. Antagonizes sensitive CYP3A4 substrates and may antagonize sensitive CYP2C9 substrates; use alternatives or monitor for efficacy if use unavoidable. Concomitant itraconazole or ketoconazole: not recommended. May decrease concentrations of hormonal contraceptives; consider alternatives.

Adverse Reactions:

Fatigue, arthralgia, leukocytosis, diarrhea, edema, nausea, dyspnea, mucositis, QT prolongation, rash, cough, decreased appetite, myalgia, constipation, pyrexia, lab abnormalities; differentiation syndrome, tumor lysis syndrome, Guillain-Barré syndrome.

Generic Availability:

NO

How Supplied:

Tabs—60

Pricing for TIBSOVO

250mg tablet (Qty: 60)
Appx. price $29276
GoodRx