Futibatinib is an oral small molecule kinase inhibitor that irreversibly binds to fibroblast growth factor receptors (FGFRs) 1, 2, 3, and 4, inhibiting their phosphorylation and downstream signaling pathways, thereby blocking tumor cell proliferation and survival.

1、 Drug name and main ingredients

1. Common name: Futibatinib

2. Product Name: LYTGOBI ®

3. Dosage form: Oral film coated tablets

4. Main ingredients: Each tablet contains 4mg of Fubatinib

2、 Indications

Cholangiocarcinoma: Used to treat adult patients with unresectable locally advanced or metastatic intrahepatic cholangiocarcinoma who have previously received treatment, and whose tumors carry fibroblast growth factor receptor 2 (FGFR2) gene fusion or other rearrangements. This indication is based on accelerated approval of objective response rate (ORR) and duration of response (DOR), and subsequent confirmatory trials may be needed to confirm clinical benefits.

3、 Specifications and characteristics

1. Specification: 4mg/tablet, round white film coated tablet, with "4MG" engraved on one side and "FBN" on the other side.

2. Packaging: 7-day dose packaging (35 tablets/box, 28 tablets/box, or 21 tablets/box, corresponding to different dose regimens).

4、 Usage and dosage

1. Recommended dosage: 20mg per day (5 tablets in 4mg format), taken orally once until disease progression or intolerable toxicity occurs.

2. Usage: Swallow the whole tablet, it can be taken with food or on an empty stomach, and take the medication at a fixed time every day.

3. Omission treatment: If the missed dose exceeds 12 hours, skip the dose and take it according to the original plan the next day; No need to take additional medication after vomiting.

5、 Dose adjustment

1. First dose reduction: 16mg (4 tablets) once daily;

2. Secondary reduction: 12mg (3 tablets) once daily;

3. Permanent discontinuation of medication: If unable to tolerate a dose of 12mg.

4. Adjustment basis:

Hyperphosphatemia: When blood phosphorus levels exceed 7mg/dL, treatment should be reduced or interrupted;

Other adverse reactions: Suspend or adjust the dosage according to the severity (such as suspending to restore to level 1 toxicity for level 3 toxicity).

6、 Medication precautions

1. Eye toxicity: May cause retinal pigment epithelial detachment (RPED), regular ophthalmic examinations (including OCT) should be performed before and during treatment, and urgent medical attention should be sought if symptoms such as blurred vision occur.

2. Hyperphosphatemia: 88% of patients experience elevated blood phosphorus levels, requiring monitoring of blood phosphorus levels and treatment with a low phosphorus diet or phosphate binders.

3. Dietary taboos: Avoid grapefruit juice (which may interfere with metabolism).

7、 Medication for special populations

1. Pregnant women: prohibited, animal experiments show embryotoxicity.

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within one week of discontinuation of medication.

3. Liver dysfunction: Moderate to severe liver injury (Child Pugh B/C) requires dose adjustment or discontinuation.

4. Children: Safety has not been established.

8、 Adverse reactions

1. Common (≥ 20%): Nail toxicity (47%), musculoskeletal pain (43%), constipation (39%), diarrhea (39%), fatigue (37%), dry mouth (35%), hair loss (34%), and oral inflammation (30%).

2. Laboratory abnormalities: hyperphosphatemia (97%), elevated serum creatinine (58%), low hemoglobin (52%), elevated liver enzymes (50%).

9、 Contraindications

There are no absolute contraindications, but it is contraindicated for use in combination with potent P-gp/CYP3A inhibitors (such as itraconazole) or inducers (such as rifampicin).

10、 Drug interactions

1. P-gp/CYP3A inhibitors: increase exposure to Fubatinib and avoid combination therapy;

2. P-gp/CYP3A inducer: reduce the efficacy of Fubatinib and avoid combination therapy;

3. P-gp/BCRP substrates: may increase the toxicity of combination drugs and need to be monitored.

11、 Storage method

Store at room temperature (20-25 ° C), avoid light and moisture, and store in original packaging.

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