futibatinib

High Alert

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

Contraind./Precautions ⬆ ⬇

Contraindicated in:

OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Cirrhosis or total bilirubin >1.5–3 times upper limit of normal (↑ risk of hepatotoxicity);
Rep: Women of reproductive potential and men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

Derm: alopecia, dry skin, nail discoloration, nail hypertrophy, nail infection, palmar-plantar erythrodysesthesia syndrome

EENT: dry eyes, blurred vision, retinal pigment epithelial detachment

Endo: hyperglycemia, hypoglycemia

F and E: hypercalcemia, hyperkalemia, hyperphosphatemia, hypokalemia, hyponatremia, hypophosphatemia

GI: abdominal pain, constipation, diarrhea, dry mouth, hyperbilirubinemia, hypoalbuminemia, nausea, stomatitis, vomiting, ↑liver enzymes, ascites, bile duct obstruction, GI BLEEDING

GU: ↑serum creatinine, urinary tract infection

Hemat: ↑aPTT, ↑INR, anemia, leukopenia, lymphocytopenia, neutropenia, thrombocytopenia

Metab: ↓appetite, weight loss

MS: ↑CK, arthralgia, pain

Neuro: dysgeusia, fatigue

Misc: fever

Interactions ⬆ ⬇

Drug-drug:

Dual P-glycoprotein (P-gp) inhibitors and strong CYP3A inhibitors, including itraconazole, may ↑ levels and risk of toxicity; avoid concurrent use.
Dual P-gp inducers and strong CYP3A inducers, including rifampin, may ↓ levels and effectiveness; avoid concurrent use.
May ↑ levels and risk of toxicity of P-gp substrates.
May ↑ levels and risk of toxicity of breast cancer resistance protein substrates.

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

PO (Adults ): 20 mg once daily until disease progression or unacceptable toxicity.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

FGFR kinase inhibitor that binds to and inhibits FGFR1, FGFR2, FGFR3, and FGFR4 enzyme activity, which results in decreased FGFR-related signaling and decreased cell viability in cancer cell lines expressing FGFR genetic alterations, including point mutations, amplifications, and fusions.

Therapeutic effects:

Decreased progression of locally advanced or metastatic intrahepatic cholangiocarcinoma.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: kinase inhibitors, fibroblast growth factor receptor inhibitor

Pharmacokinetics ⬆ ⬇

Absorption: Rapidly absorbed; extent of absorption unknown.

Distribution: Extensively distributed to tissues.

Protein Binding: 95%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme and to a lesser extent by the CYP2C9 and CYP2D6 isoenzymes. Primarily excreted in feces (91%), with 9% excreted in urine; negligible amount excreted as unchanged drug.

Half-Life: 2.9 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	2 hr	24 hr

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care professional if visual changes occur. Advise on the use of artificial tears or hydrating eye gels to prevent or treat dry eyes.
Advise patient to notify health care professional if symptoms of hyperphosphatemia (muscle cramps, numbness or tingling around mouth) occur.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: May cause fetal harm. Advise patient notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Advise women of reproductive potential and men with female partners of reproductive potential to use effective contraception. Advise patient to not breastfeed during and for 1 wk after last dose.

Pronunciation ⬆ ⬇

Code ⬆

NDC Code

63069- PENN PHARMACEUTICAL SERVICES LIMITED
- 63069-101-
  - 63069-101-01- 12500 TABLET in 1 DRUM (63069-101-01)

64842- TAIHO PHARMACEUTICAL CO., LTD.
- 64842-0120- LYTGOBI
  - 64842-0120-4- 1 BLISTER PACK in 1 CARTON (64842-0120-4) / 21 TABLET in 1 BLISTER PACK

64842- TAIHO PHARMACEUTICAL CO., LTD.
- 64842-0120- LYTGOBI
  - 64842-0120-5- 1 BLISTER PACK in 1 CARTON (64842-0120-5) / 28 TABLET in 1 BLISTER PACK

64842- TAIHO PHARMACEUTICAL CO., LTD.
- 64842-0120- LYTGOBI
  - 64842-0120-6- 1 BLISTER PACK in 1 CARTON (64842-0120-6) / 35 TABLET in 1 BLISTER PACK

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Indications ⬇