Colorectal and other GI cancers:
Indications for PEMAZYRE:
In adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement as detected by an FDA-approved test.
Confirm presence of an FGFR2 fusion or rearrangement prior to initiation. Swallow whole. 13.5mg once daily for 14 consecutive days, followed by 7 days off therapy, in 21-day cycles. Continue until disease progression or unacceptable toxicity. Concomitant strong or moderate CYP3A4 inhibitors (if unavoidable): reduce from 13.5mg to 9mg once daily, or reduce from 9mg to 4.5mg once daily. Severe renal or severe hepatic impairment: 9mg once daily for 14 consecutive days, followed by 7 days off therapy, in 21-day cycles. Dose modifications for adverse reactions: see full labeling.
Risk of retinal pigment epithelial detachment. Perform eye exam prior to initiation, every 2 months for the first 6 months, then every 3 months thereafter; if visual symptoms develop, evaluate immediately. Monitor for hyperphosphatemia (can lead to soft tissue mineralization, cutaneous calcification, others). Initiate a low phosphate diet if serum phosphate >5.5mg/dL; if serum phosphate >7mg/dL, initiate phosphate lowering therapy and withhold, reduce dose, or permanently discontinue Pemazyre based on duration and severity. Severe renal impairment (GFR <30mL/min). Severe hepatic impairment (total bilirubin >3×ULN with any AST). Embryo-fetal toxicity. Advise females of reproductive potential and males (w. female partners) to use effective contraception during and for 1 week after the last dose. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended (during and for 1 week after the last dose).
Potentiated by strong or moderate CYP3A4 inhibitors; avoid concomitant use; if unavoidable, reduce dose (see Adults). Antagonized by strong or moderate CYP3A4 inducers; avoid use.
Hyperphosphatemia, alopecia, diarrhea, nail toxicity, fatigue, dysgeusia, nausea, constipation, stomatitis, dry eye, dry mouth, decreased appetite, vomiting, arthralgia, abdominal pain, hypophosphatemia, back pain, dry skin; lab abnormalities, ocular toxicity.
Generic Drug Availability: