Jubilant Therapeutics Inc. Reports Development of Orally Available and Brain Penetrant Small Molecule Inhibitors of PD-L1 at the 2022 American Society of Clinical Oncology (ASCO) Annual Meeting
BEDMINSTER, N.J., June 1, 2022 /PRNewswire/ -- Jubilant Therapeutics Inc. a clinical stage precision therapeutics Company advancing small molecule therapeutics to address unmet medical needs in oncology and autoimmune diseases, today announced data to be presented at the 2022 American Society of Clinical Oncology (ASCO) Annual Meeting. The data report on the pharmacokinetic and in vitro and in vivo anti-cancer properties of JBI-2174, the Company's lead oral, brain penetrant PD-L1 inhibitor, which is in IND-enabling studies for the treatment for solid tumors. The poster will be presented by Luca Rastelli, Ph.D., Company's Chief Scientific Officer, during the Developmental Therapeutics — Immunotherapy session at 8:00 a.m. CDT on June 05, 2022. The abstract is available here.
"Checkpoint inhibitors, such as anti-PD-1 and anti-PDL1 antibodies, have revolutionized cancer treatment by enabling the immune system to attack tumor cells," said Luca Rastelli. "However, these antibodies have poor brain penetrance and shown limited efficacy in brain cancers. Employing our structure-based drug design and computational algorithms, we have designed oral small molecule checkpoint inhibitors that address this limitation. We are focused on completing our IND-enabling studies and hope to initiate shortly the clinical trials with JBI-2174 in patients with specific brain tumors." he further added.
The potency, pharmacokinetics and in vivo activity of rationally designed small molecule inhibitors of PD-L1 were evaluated. The Company's lead anti-PD-L1 candidate, JBI-2174, demonstrated strong affinity for PD-L1 with an IC50 of approximately 1 nM. In selectivity assays for immune-oncology targets, JBI-2174 was highly selective for PD-L1 and also inhibited PD-L1/PD-1 mediated signaling essential for T-cell modulation. In multiple animal models where tumor cells were injected in the brain, JBI-2174 demonstrated sustained brain exposure, efficacy equivalent to an anti-PD-L1 antibody and increased survival compared to control. The results suggest an orally administered brain penetrant small molecule PD-L1 inhibitor could achieve efficacy in brain tumors that do not usually respond to immune-checkpoint antibodies
About Jubilant Therapeutics Inc.
Jubilant Therapeutics Inc. is a clinical stage precision therapeutics Company advancing potent and selective small molecule modulators to address unmet medical needs in oncology and autoimmune diseases. Its advanced discovery engine integrates structure-based design and computational algorithms to discover and develop novel, precision therapeutics against both first-in-class and validated but intractable targets in genetically defined patient populations. The Company's advanced program - first in class dual inhibitor of LSD1/HDAC6 has entered Phase I/IIa clinical trials to treat solid tumors, followed by additional INDs with novel brain-penetrant modulators of PRMT5 and PDL1, as well as PAD4 inhibitors in oncology and inflammatory indications. Jubilant Therapeutics Inc. is headquartered in Bedminster, NJ and guided by globally renowned key opinion leaders and scientific advisory board members. For more information, please visit www.jubilanttx.com or follow us on Twitter @JubilantTx and LinkedIn.
SOURCE Jubilant Therapeutics Inc.
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