Selpercatinib shows activity in gastrointestinal tumours: Eli Lilly

April 17, 2021 0 By FM

Selpercatinib (Retevmo) treatment showed promising new antitumour activity and safety in various RET fusion-positive advanced solid tumours, according to Eli Lilly and Company’s phase I/II LIBRETTO-001 trial results. The latest data showed that the activity of the drug is beyond lung and thyroid cancers and includes multiple treatment-refractory gastrointestinal (GI) malignancies as well.

Selpercatinib is a selective and potent RET kinase inhibitor. It inhibits wild-type, mutant and fusion products involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET), with potential antineoplastic activity.

Selpercatinib is currently used for the treatment of non-small cell lung cancer, medullary thyroid cancer, and other types of thyroid cancers in people whose tumours have an alteration in a specific gene. The oral drug has been granted US FDA approval in May 2020 for treating certain patients with thyroid cancer or non-small cell lung cancer.

The recent phase I/II LIBRETTO-001 trial enrolled 32 adult patients with 12 unique RET fusion-positive advanced cancer types including pancreatic, colon, breast, salivary, sarcoma, carcinoid, rectal neuroendocrine, small intestine, xanthogranuloma, ovarian, pulmonary carcinosarcoma, and unknown primary cancers.

The study is conducted in 16 countries at 89 sites and has a dose-escalation phase (phase 1) and a dose-expansion phase (phase 2). Data from the trial showed that a confirmed objective response rate (ORR) of 47% was observed in all subjects with confirmed responses noted in nine unique RET fusion-positive advanced cancer types. ORR is referred to the proportion of patients with tumour size reduction of a predefined amount and for a minimum time period.

With a 13-month median follow-up period, the median duration of response (DoR), which is the time from response (R) to progression/death (P/D), was not reached, while responses were progressing in 73% of the responding subjects. Furthermore, safety among the trial subjects in this cohort was in line with selpercatinib’s already established safety profile, said the company.

The trial is currently enrolling patients with RET-altered tumours which are beyond lung cancer.