Ascletis Pharma has dosed the first subject in the Phase I clinical trial of its ASC61 to treat advanced solid tumours in the US.
The dose-escalation study will analyse the safety and tolerability of ASC61.
It is also intended to define the maximum tolerated dose (MTD) and recommended Phase II dose (RP2D) of the drug in advanced solid tumour patients who have progressed during or after standard therapy.
Being carried out at Nebraska Cancer Specialists and California Cancer Centers, the trial is anticipated to conclude in March next year.
ASC61 is an oral PD-L1 small molecule inhibitor prodrug.
The active metabolite of the therapy, ASC61-A, is an inhibitor that hinders PD-1/PD-L1 interaction by stimulating PD-L1 dimerisation and internalisation.
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In a head-to-head comparison study, treatment with ASC61-A elicited IFNγ secretion in a concentration-dependent way with an EC50 of 2.86 nM.
Furthermore, ASC61-A-induced IFNγ levels were in line with those of Keytruda.
ASC61 as a monotherapy showed to offer substantial antitumor efficacy in various animal models including humanised mouse model.
According to the preclinical studies, ASC61 demonstrated to have good safety and pharmacokinetic profiles in animal models.
Ascletis founder, chairman and CEO Dr Jinzi Wu said: “Immunogenicity and the poor permeability of tumour tissues are the major disadvantages of therapeutic antibodies, which can cause a low response rate of PD-1/PD-L1 antibodies.
“As a highly differentiated small molecule PD-L1 inhibitor, ASC61 has several advantages over antibodies and showed promising preliminary efficacy and safety profile in preclinical studies.
“This progress of ASC61 on advanced solid tumours further demonstrated Ascletis’ global R&D capability and execution.”
The latest development comes after the company obtained clearance from the US Food and Drug Administration for its Investigational New Drug (IND) application for ASC10 to conduct a Phase Ib trial for Covid-19.