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ARQ 087 appears safe for treatment of intrahepatic cholangiocarcinoma
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ARQ 087, a multi-kinase inhibitor designed to inhibit fibroblast growth factor receptor, displayed a favorable safety profile when administered as monotherapy to patients with intrahepatic cholangiocarcinoma, according to data presented at the European Society of Medical Oncology 18th World Congress on Gastrointestinal Cancer.
“Intrahepatic cholangiocarcinoma is a rare liver cancer with a high mortality rate and limited treatment options,” Brian Schwartz, MD, head of research and development and chief medical officer at ArQule, said in a press release. “There is scientific evidence that this disease can be caused by a number of different genetic alterations, one being [fibroblast growth factor receptor], thus making the use of precision medicine essential in treating these patients. The data we presented, while preliminary, are very encouraging and offer evidence that ARQ 087 is active in those patients with a [fibroblast growth factor receptor 2] genetic alteration.”
In the phase 1/2 dose escalation trial, researchers dosed 21 patients with advanced or metastatic intrahepatic cholangiocarcinoma (iCCA) with either 300 mg or 400 mg of ARG 087 (ArQule).
In part one of the study, safety and tolerability were addressed and in part two, the safety and tolerability with fibroblast growth factor receptor (FGFR) — a genetic translocation that has been implicated in the development and progression of iCCA — including FGFR2 fusion, is addressed. The researchers note that part two of the study is ongoing.
Of all the patients, 20 reported next generation sequencing or fluorescence in situ hybridization, of which 14 presented with FGFR2 genetic alterations. Twelve of the 14 patients with FGFR2 fusion had data evaluable for evaluation.
The objective response rate was 25% (three partial responses) and the disease control rate was 75% (three partial responses and six patients with stable disease).
Twenty-five percent of patients had minor responses and showed reduced tumor burden (between 15% and 29%; n =3). In addition, disease control was observed in 50% of patients (n = 6) and progressive disease was the best response in 25% of patients.
The most common adverse events were grade 1 or 2 in nature and every patient experienced at least one. Grade 3 or greater adverse events experienced by patients consisted of fatigue (5%), increased alanine aminotransferase levels (5%), increased aspartate transferase levels (10%), blurry vision (5%), vomiting (5%), stomatitis (5%) and anemia (5%).
“Further development of ARQ 087 as monotherapy or in combination with other anti-cancer agents as second or first line therapy for patients with iCCA with FGFR2 fusion is deemed feasible considering its favorable safety profile and preliminary evidence of anti-cancer activity,” the researchers concluded.
Reference:
Mazzaferro V, et al. Abstract #340. Presented at: European Society of Medical Oncology World Congress on Gastrointestinal Cancer; June 29-July 2, 2016; Barcelona, Spain.
Disclosure: Schwartz is employed by ArQule.