Tolero Pharmaceuticals has dosed the first patient in a Phase l trial to examine TP-0184 for the treatment of patients with advanced solid tumours.

The open-label, dose-escalation trial is intended to analyse the safety, pharmacokinetics, and pharmacodynamics of oral daily doses of TP-0184 for the first 21 days of a 28-day cycle.

Around 40 subjects are expected to be enrolled in the trial, which is being carried out at sites in the US.

The trial’s primary objective is to determine the maximum tolerated dose (MTD) and dose-limiting toxicities (DLTs) of TP-0184.

Its secondary objectives are to analyse the pharmacokinetics and pharmacodynamics of TP-0184, observe patients for any evidence of anti-tumour activity of TP-0184 by objective radiographic assessment, and determine the recommended Phase ll dose for future studies of TP-0184.

“The initiation of this study of TP-0184 represents an important milestone for Tolero Pharmaceuticals.”

Tolero Pharmaceuticals CEO David Bearss said: “The initiation of this study of TP-0184 represents an important milestone for Tolero Pharmaceuticals, as it marks the second investigational agent from our development programme to enter the clinical research stage this year.

“We look forward to understanding more about the profile of TP-0184 and its role in inhibiting activin A receptor type 1 (ACVR1), which is mutated in approximately 1-4% of solid tumours and 32% of diffuse intrinsic pontine gliomas (DIPGs), an aggressive form of pediatric brain cancer.”

TP-0184 is small molecule inhibitor of ACVR1, which is an activin A receptor type 1 (ACVR1) inhibitor.

The investigational drug is involved in the transforming growth factor beta (TGFβ) signalling pathway.