Bone and connective tissue cancer:
Indications for: TURALIO
In adults with symptomatic tenosynovial giant cell tumor (TGCT) associated with severe morbidity or functional limitations and not amenable to improvement with surgery.
Adult Dosage:
Swallow whole. Take with a low-fat meal (~11–14g of total fat). 250mg twice daily until disease progression or unacceptable toxicity. Mild to severe renal impairment (CrCl 15–89mL/min): 125mg in the AM and 250mg in the PM. Moderate hepatic impairment (total bilirubin >1.5–3×ULN, not due to Gilbert’s syndrome, with any AST): 125mg twice daily. Dose modifications for adverse reactions, concomitant moderate or strong CYP3A or UGT inhibitors, acid-reducing agents: see full labeling.
Children Dosage:
Not established.
Boxed Warning:
Hepatotoxicity.
TURALIO Warnings/Precautions:
Risk of liver injury (may be fatal). Avoid in patients with pre-existing increased serum transaminases, total/direct bilirubin >ULN, or active liver or biliary tract disease, including increased ALP. Monitor LFTs prior to initiation, weekly for the first 8 weeks, every 2 weeks for the next month, and then every 3 months thereafter. Withhold and reduce dose or permanently discontinue based on severity of hepatotoxicity. Severe hepatic impairment (total bilirubin >3–10×ULN and any AST): not studied. Embryo-fetal toxicity. Advise use of effective contraception during and for 1 month (females; use non-hormonal method) or for 1 week (males w. female partners) after last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after last dose).
TURALIO Classification:
Kinase inhibitor.
TURALIO Interactions:
Avoid coadministration with a high-fat meal. Avoid concomitant other products known to cause hepatotoxicity. May be potentiated by moderate or strong CYP3A (including grapefruit or grapefruit juice) or UGT inhibitors; avoid; if unavoidable, reduce Turalio dose. Antagonized by strong CYP3A inducers (including St. John's wort) or proton pump inhibitors (alternatively, can use antacids or H2-blockers); avoid. Antagonizes CYP3A substrates (eg, hormonal contraceptives, others); avoid; if unavoidable, increase substrate dose.
Adverse Reactions:
Increased lactate dehydrogenase, hair color changes, fatigue, increased AST, decreased neutrophils, increased cholesterol, decreased lymphocytes, eye edema, increased ALP, increased ALT, decreased hemoglobin, rash, dysgeusia, decreased phosphate.
Drug Elimination:
Fecal (65%), renal (27%).
REMS:
Generic Drug Availability:
NO
How Supplied:
Caps—28, 120
