Ailingda Fanregratinib Tartrate Tablets

1. Indications and Usage
Fanregratinib tartrate tablets are indicated for the treatment of adult patients with previously treated, locally advanced, metastatic, or unresectable intrahepatic cholangiocarcinoma harboring fibroblast growth factor receptor 2 (FGFR2) fusions or rearrangements.
Patient selection should be based on confirmation of FGFR2 fusion or rearrangement by a validated diagnostic test.
2. Dosage and Administration
Route: Oral administration.
Dose and Schedule: The approved English dosing regimen has not been published. Dose, schedule, dose modifications, and administration instructions should follow the approved Chinese label and treating physician guidance.
Administration: Tablets should be taken orally. Whether the drug should be taken with or without food should be confirmed from the approved product label.
Dose Modifications: Dose interruption, reduction, or discontinuation may be required for adverse reactions; specific modification criteria should be obtained from the official Chinese prescribing information.
3. Mechanism of Action
Fanregratinib is a selective small-molecule inhibitor of FGFR1, FGFR2, and FGFR3.
Aberrant FGFR signaling can drive tumor cell proliferation, survival, and angiogenesis. Fanregratinib inhibits FGFR kinase activity, thereby suppressing downstream signaling in FGFR-altered tumor cells.
4. Safety and Warnings
FGFR2 Biomarker Requirement: Use should be restricted to patients with confirmed FGFR2 fusions or rearrangements.
Conditional Approval: Approval is based on tumor response and related endpoints from a single-arm study; continued approval may depend on verification of clinical benefit in confirmatory trials.
Hepatotoxicity: Monitor liver function tests regularly during treatment.
Ocular Toxicity: FGFR inhibitors may cause retinal pigment epithelial detachment or other ocular adverse events; patients should be monitored for visual symptoms.
Hyperphosphatemia and Soft Tissue Mineralization: Elevated phosphate levels may occur with FGFR inhibition.
Palmar-Plantar Erythrodysesthesia and Skin Toxicity: Hand-foot skin reaction, rash, and dry skin may occur.
Embryo-Fetal Toxicity: May cause fetal harm; effective contraception is recommended during treatment and for a period after the last dose.
5. Adverse Reactions and Clinical Research
Common Adverse Reactions: Expected class-related adverse reactions include hyperphosphatemia, hepatic enzyme elevation, palmar-plantar erythrodysesthesia, rash, stomatitis, diarrhea, fatigue, decreased appetite, and ocular disorders.
Clinical Research: In a pivotal single-arm, multicenter, open-label Phase II registration cohort, fanregratinib showed an IRC-assessed objective response rate of 42.5%, a disease control rate of 83.9%, a median duration of response of 6.9 months, a median progression-free survival of 6.9 months, and a median overall survival of 16.6 months in previously treated FGFR2 fusion/rearranged intrahepatic cholangiocarcinoma.
6. Drug Interactions
Formal English drug interaction data have not been published. Clinical drug interaction studies have evaluated the effects of itraconazole, rifampin, proton pump inhibitors, and food exposure on fanregratinib pharmacokinetics.
Concomitant use of strong CYP3A inhibitors, strong CYP3A inducers, and agents that increase gastric pH should be managed according to the approved label and clinical guidance.
7. Pharmaceutical Information
International Nonproprietary Name: Fanregratinib.
Chinese Name: 酒石酸凡瑞格拉替尼片.
Brand Name: ATLED .
Development Code: HMPL-453.
Drug Class: Selective oral FGFR1/2/3 inhibitor.
Dosage Form: Oral tablets.
Approval: Conditionally approved by China NMPA in 2026 for previously treated FGFR2 fusion/rearranged intrahepatic cholangiocarcinoma.
Storage and Handling: Refer to the approved Chinese package insert for strength, excipients, storage conditions, and shelf life.