Infigratinib

Infigratinib (Infigratinib) Instructions

Generic name: Infigratinib

Trade name: Truseltiq

All names: Infigratinib, Infigratinib, Truseltiq

Indications:

Indicated for the treatment of previously treated, unresectable locally advanced or metastatic cholangiocarcinoma, accompanied by fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement tested with FDA approval.

Usage and dosage:

Take 125 mg orally daily for 21 days, then stop for 7 days, with a cycle of 28 days, until disease progression or unacceptable toxicity.

Adverse reactions:

The most common adverse reactions (incidence ≥20%): nail toxicity, stomatitis, dry eye syndrome, fatigue, alopecia, palmoplantar erythema sensory syndrome, joint pain, dysgeusia, constipation, abdominal pain, dry mouth, eyelash changes, diarrhea, dry skin, loss of appetite, blurred vision and vomiting.

Contraindications:

None

Precautions:

Ocular toxicity: Infigratinib can cause retinal pigment epithelial detachment (RPED). A comprehensive eye examination, including optical coherence tomography (OCT), was performed before initiation of infigratinib treatment and at 1 month, 3 months, and every 3 months thereafter.

Hyperphosphatemia and soft tissue mineralization: Increased phosphate levels can lead to hyperphosphatemia, leading to soft tissue mineralization, cutaneous calcinosis, non-uremic calcinosis, vascular calcification, and cardiac calcification. Stop, reduce dose, or permanently discontinue medication as recommended.

Embryo-fetal toxicity: Can cause harm to the fetus. Inform patients of the potential reproductive risks and potential risks to the fetus and to use effective contraception.

Storage:

Store within the temperature range of 20°C to 25°C (68°F to 77°F), with a temperature range of 15°C to 30°C (59°F to 86°F) allowed.

Mechanism of action:

Infigratinib is a small molecule ATP-competitive tyrosine kinase inhibitor of FGFR. Alterations of FGFR in tumors can lead to constitutive FGFR signaling that supports the proliferation and survival of malignant cells.

Infigratinib blocks downstream signaling cascades by selectively binding and inhibiting FGFR activity. It induces tumor cell death by reducing cancer cell proliferation.

Safety and Efficacy:

At the 2020 ASCO meeting, a clinical study on infigratinib was released. This is a phase 2, multi-center, single-arm trial clinical study designed to study the efficacy of infigratinib as a third-line or above treatment for patients with FGFR2 fusion-positive cholangiocarcinoma.

The trial results showed that in the case of second-line treatment, the median PFS of patients was 4.63 months; the median PFS of patients who received third-line or above treatment with Infigratinib was 6.77 months. In terms of objective response rate (ORR), infigratinib’s ORR was 21.6% in patients who received third-line or above treatment.

In patients with cholangiocarcinoma with FGFR2 fusion, infigratinib has greater benefit in PFS and ORR compared with second-line standard chemotherapy regimens in third-line and above treatments.