GRC54276 has been well tolerated at the dose levels tested and has shown antitumor activity when administered as monotherapy to Hodgkin's lymphoma, colon carcinoma and buccal mucosal carcinoma patients. GRC54276 will be further tested in select patients as monotherapy and in combination with pembrolizumab or atezolizumab. Lymphoma, Targeted therapy, Hodgkin's lymphoma, Cancer immunotherapy
over 1 year ago
Clinical • P1 data • PK/PD data • Metastases
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BLNK (B Cell Linker) • LCP2 (Lymphocyte cytosolic protein 2)
In vivo efficacy was demonstrated in syngeneic mouse tumor models, both as a single agent and combination with immune check-point blockers (ICB), mouse anti-CTLA4 antibody or Atezolizumab (human anti-PD-L1 antibody). The no observed adverse effect levels in the 14-day and 17-day exploratory studies in mice and monkeys were 50 and 15 mg/kg/day, respectively.Conclusions GRC 54276, our clinical candidate is potent, selective, orally bioavailable HPK1 inhibitor demonstrating strong single-agent and combination efficacy, low DDI liability accompanied by acceptable early safety profile in mice and monkeys. GRC 54276 is undergoing IND enabling studies to advance to Phase 1 clinical trial.
almost 3 years ago
Clinical
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IFNG (Interferon, gamma) • IL2 (Interleukin 2) • CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)