Tinengotinib shows promising activity against cholangiocarcinoma

In patients with cholangiocarcinoma with FGFR2 fusions that progressed following FGFR inhibitor therapy, tinengotinib has demonstrated potential antitumour activity in a phase II study.

The study included 55 adult cholangiocarcinoma patients (median age 61 years, 56 percent female) who had previous systemic chemotherapy and an ECOG score of 0–1. Patients were grouped according to their FGFR status, as follows: FGFR2 fusions with primary FGFR inhibitor resistance (cohort A1, n=18), FGFR2 fusions with acquired FGFR inhibitor resistance (cohort A2, n=11), other FGFR alterations (cohort B, n=13), FGFR wild-type (cohort C, n=13).

All patients received tinengotinib 10 mg, which was administered orally daily in 28-day treatment cycles until documented disease progression, unacceptable toxicity, or withdrawal of consent. The primary endpoint was objective response rate (ORR) as per investigator assessment. Safety was also evaluated.

Over a median follow-up of 11.3 months, the ORR was 6.3 percent in cohort A1, 30 percent in cohort A2, 23.1 percent in cohort B, and 0 percent in cohort C.

Grade 3 treatment-related adverse events (TRAEs) included hypertension in 31 percent of patients, palmar-plantar erythrodysesthesia syndrome in 13 percent, and stomatitis in 11 percent. Grade 4 TRAEs occurred in 4 percent of patients, including a case of increased lipase and a case of posterior reversible encephalopathy syndrome. None of the patients experienced any grade 5 TRAEs.