Tasfigo succinate is a novel tyrosine kinase inhibitor that exerts anti-tumor effects by targeting FGFR1/2/3, mainly used for the treatment of biliary tract cancer with FGFR2 gene abnormalities.

1. Mechanism of action

Succinate sulfatinib selectively inhibits the tyrosine kinase activity of FGFR1, FGFR2, and FGFR3 in the fibroblast growth factor receptor (FGFR) family, blocking downstream signaling pathways and thereby inhibiting tumor cell proliferation and survival.

2. Clinical application

(1) Indications

Approved for the treatment of unresectable biliary tract cancer patients who have progressed after chemotherapy and carry FGFR2 gene fusion or rearrangement.

(2) Usage and dosage

The recommended dosage for adults is 140mg once a day, taken orally on an empty stomach, and the entire tablet should be swallowed. Dose adjustment can be made based on adverse reactions, such as hyperphosphatemia, which requires medication suspension until recovery.

(3). Medication for special populations

(3.1) Pregnancy and lactation

Pregnant women are only allowed to use it when there is significant benefit; Prohibited during lactation period; People of childbearing age should strictly use contraception during the medication period and within 6 days after discontinuation.

(3.2) Liver dysfunction

Mainly metabolized by the liver, patients with moderate to severe damage need to adjust the dosage carefully to avoid drug accumulation and increased toxicity.

(3.3) Child patients

Safety and efficacy data for individuals under the age of 18 have not yet been established, and it is not recommended to use it.

(4) Drug interactions

This drug is a substrate for P-gp and CYP3A, and interacts with drugs such as rifampicin; Simultaneously, it may inhibit enzyme systems such as CYP3A and CYP4F12.

(5). Adverse reaction management

(5.1) Common reactions

Diarrhea (33.3%), stomatitis (24.6%) and other gastrointestinal symptoms; 72.5% developed nail diseases, and 49.3% developed palmar and plantar redness and swelling syndrome.

(5.2) Hematotoxicity

Monitoring of thrombocytopenia, neutropenia, etc. is required. For grade 3, the medication needs to be discontinued until ≤ grade 2, and then reduced and restored. For grade 4, the medication needs to be permanently discontinued.

(5.3) Eye lesions

Dry eye syndrome, keratitis, and other conditions require regular eye examinations. For intolerable grades 2 or 3, medication should be temporarily suspended and reduced for recovery.