Theseus Pharmaceuticals has treated the first subject in the Phase I segment of its Phase I/II clinical trial to assess THE-630 in advanced gastrointestinal stromal tumour (GIST) patients.

A pan-variant receptor tyrosine kinase KIT inhibitor, THE-630 is intended for individuals with advanced GIST whose tumour is resistant to prior lines of treatment due to mutations. 

The multicentre, open-label, first-in-human dose-escalation and expansion trial will assess the pharmacokinetics, safety and anti-tumour activity of oral THE-630. 

The dose escalation or Phase I portion of the trial will have subjects with unresectable or metastatic GIST whose disease progressed on or are intolerant to treatment with imatinib.

These patients were also treated with at least one of four therapies, namely sunitinib, regorafenib, ripretinib or avapritinib. 

The primary goal of this phase is to assess THE-630’s safety profile, including dose-limiting toxicities, maximum tolerated dose, and the recommended dose for the Phase II trial.

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By GlobalData

On determining the recommended dose, the expansion phase or the Phase II portion will enrol unresectable or metastatic GIST patients into groups based on their previous treatment from a second-line to a fifth-line population. 

The primary goal of this portion is to analyse the therapy’s anti-tumour activity in trial subjects.

Preliminary results from the Phase I segment of the trial are anticipated to be published in the first half of next year.

Theseus Pharmaceuticals chief medical officer David Kerstein said: “The initiation of our Phase I/II trial in patients with previously-treated advanced GIST is an important milestone as we begin to characterise THE-630 in the clinic. 

“We believe THE-630 has a differentiated profile of pan-variant activity against KIT and we look forward to exploring a number of GIST settings where pan-variant inhibition may translate into meaningful clinical benefit – from the fifth-line, where no standard therapies exist, to earlier lines of therapy such as the second-line, where the current standard of care yields less than optimal outcomes.”

Last week, First Wave BioPharma concluded enrolment of subjects for the second part of the Phase II RESERVOIR clinical trial of FW-COV to treat gastrointestinal infections associated with Covid-19.