Select therapeutic use:

Colorectal and other GI cancers:

Indications for: TIBSOVO

Previously treated, locally advanced or metastatic cholangiocarcinoma with an isocitrate dehydrogenase-1 (IDH1) mutation as detected by an FDA-approved test.

Adult Dosage:

Swallow whole. Take at same time each day. Avoid a high-fat meal. 500mg once daily until disease progression or unacceptable toxicity. 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 Dosage:

Not established.

Boxed Warning:

Differentiation syndrome in AML.

TIBSOVO Warnings/Precautions:

Risk of differentiation syndrome in AML (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. 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. Obtain ECGs prior to treatment, at least weekly for the first 3 weeks, and then once monthly thereafter. For AML: 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 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 the last dose).

TIBSOVO Classification:

Isocitrate dehydrogenase-1 (IDH1) inhibitor.

TIBSOVO 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, abdominal pain, ascites, anemia, lab abnormalities; tumor lysis syndrome, Guillain-Barré syndrome.

Generic Drug Availability:

NO

How Supplied:

Tabs—60

Pricing for TIBSOVO

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

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 Dosage:

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 Dosage:

Not established.

Boxed Warning:

Differentiation syndrome in AML.

TIBSOVO Warnings/Precautions:

Risk of differentiation syndrome in AML (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. 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. Obtain ECGs prior to treatment, at least weekly for the first 3 weeks, and then once monthly thereafter. For AML: 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 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 the last dose).

TIBSOVO Classification:

Isocitrate dehydrogenase-1 (IDH1) inhibitor.

TIBSOVO 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, abdominal pain, ascites, anemia, lab abnormalities; tumor lysis syndrome, Guillain-Barré syndrome.

Generic Drug Availability:

NO

How Supplied:

Tabs—60

Pricing for TIBSOVO

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