Colorectal and other GI cancers:

Indications for: LYTGOBI

In adults with previously treated, unresectable, locally advanced or metastatic intrahepatic cholangiocarcinoma harboring fibroblast growth factor receptor 2 (FGFR2) gene fusions or other rearrangements.

Adult Dosage:

Confirm presence of FGFR2 gene fusion or rearrangement prior to initiation. Swallow whole. 20mg (5 tabs) once daily until disease progression or toxicity occurs. Dose modifications for adverse reactions: see full labeling.

Children Dosage:

Not established.

LYTGOBI Warnings/Precautions:

Risk for retinal pigment epithelial detachment. Perform eye exam prior to initiation, every 2 months for the 1st 6 months, then every 3 months thereafter; if visual symptoms develop, evaluate immediately. Monitor for hyperphosphatemia (can lead to soft tissue mineralization, vascular calcification, others). Initiate a low phosphate diet and phosphate lowering therapy if serum phosphate ≥5.5mg/dL. If serum phosphate >7mg/dL, initiate or increase phosphate lowering therapy and withhold, reduce dose, or permanently discontinue Lytgobi based on duration and severity. 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).

LYTGOBI Classification:

Kinase inhibitor.

LYTGOBI Interactions:

May be potentiated by dual P-gp and strong CYP3A inhibitors; avoid concomitant use. May be antagonized by dual P-gp and strong CYP3A inducers; avoid concomitant use. May potentiate P-gp or BCRP substrates; monitor and reduce doses. 

Adverse Reactions:

Nail toxicity, musculoskeletal pain, constipation, diarrhea, fatigue, dry mouth, alopecia, stomatitis, abdominal pain, dry skin, arthralgia, dysgeusia, dry eye, nausea, decreased appetite, urinary tract infection, palmar-plantar erythrodysesthesia syndrome, vomiting, lab abnormalities; pyrexia, GI hemorrhage.

Metabolism:

Primarily by CYP3A and to a lesser extent by CYP2C9 and CYP2D6 in vitro. 

Drug Elimination:

Fecal (91%), renal (9%). Half-life: 2.9 hours. 

Generic Drug Availability:

NO

How Supplied:

Blister cards—21, 28, 35