General Information

Truseltiq (infigratinib) is an orally administered, ATP-competitive, tyrosine kinase inhibitor of FGFR.

Truseltiq is specifically indicated for the treatment of adults with previously treated, unresectable locally advanced or metastatic cholangiocarcinoma with a fibroblast growth factor receptor 2 (FGFR2) fusion or other rearrangement as detected by an FDA-approved test.

Truseltiq is supplied as a capsule for oral administration. The recommended dosage of Truseltiq is 125 mg (one 100 mg capsule and one 25 mg capsule) orally once daily for 21 consecutive days followed by 7 days off therapy, in 28-day cycles. Continue treatment until disease progression or unacceptable toxicity. Instruct patients to take Truseltiq on an empty stomach at least 1 hour before or 2 hours after food, at approximately the same time each day. Instruct patients to swallow capsules whole with a glass of water. Advise patients to not crush, chew, or dissolve capsules. If a dose of Truseltiq is missed by ≥4 hours or if vomiting occurs, instruct patients to resume the regular daily dose schedule for Truseltiq the next day.

Mechanism of Action

Side EffectsTruseltiq (infigratinib) is a small molecule kinase inhibitor of FGFR with IC50 values of 1.1, 1, 2, and 61 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. The major human metabolites of infigratinib, BHS697 and CQM157, have similar in vitro binding affinities for FGFR1, FGFR2, and FGFR3 compared to infigratinib. Infigratinib inhibited FGFR signaling and decreased cell proliferation in cancer cell lines with activating FGFR amplifications, mutations, or fusions. Constitutive FGFR signaling can support the proliferation and survival of malignant cells. 

Side Effects

Adverse effects associated with the use of Truseltiq may include, but are not limited to, the following:

• nail toxicity
• stomatitis
• dry eye
• fatigue
• alopecia
• palmar-plantar erythrodysesthesia syndrome
• arthralgia
• dysgeusia
• constipation
• abdominal pain
• dry mouth
• eyelash changes
• diarrhea
• dry skin
• decreased appetite
• vision blurred
• vomiting
• laboratory abnormalities

Clinical Trial Results

This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in confirmatory trial(s).

The approval of Truseltiq is based on a Phase 2 clinical study in which 108 patients who had undergone at least one prior treatment for advanced CCA received 125 mg of Truseltiq daily for 21 days of 28-day cycles. Of these patients, 107 (99%) had Stage IV CCA. All patients had received at least 1 prior line of systemic therapy. The study’s primary endpoint demonstrated a confirmed objective response rate (ORR) of 23%. The study also showed a median duration of response (DOR) of 5.0 months.