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.
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.
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).
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.
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.
Fecal (65%), renal (27%).
Generic Drug Availability: