On November 8, 2021 Tempest Therapeutics, Inc. (Nasdaq: TPST), a clinical-stage oncology company developing potentially first-in-class therapeutics that combine both targeted and immune-mediated mechanisms, reported that the U.S. Patent and Trademark Office has issued multiple patents covering composition of matter for the company’s therapeutic product candidate TPST-1495, an orally available small molecule designed to selectively block the EP2 and EP4 receptors in the prostaglandin (PGE2) pathway (Press release, Tempest Therapeutics, NOV 8, 2021, View Source [SID1234594779]).
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"We have shown in pre-clinical studies that our approach to inhibit signaling through both EP2 and EP4 receptors with our TPST-1495 dual antagonist confers significantly increased potency compared to single EP4 inhibitors, as well as improvement over other prostaglandin-inhibition approaches including NSAIDs, and could represent an important evolution in the targeting of this pathway in oncology," said Tom Dubensky, president of Tempest. "Prostaglandin signaling drives a wide range of cancers as well as resistance to immune checkpoint inhibitor therapies, so we are excited about the potential of our ongoing clinical evaluation of TPST-1495. The intellectual property portfolio covering TPST-1495 and its uses is important to protect the differentiated properties of this molecule."
The patent portfolio now includes U.S. Patent Numbers 10,968,201 and 11,066,405, as well as a number of pending applications in the United States and other markets outside of the United States. The pending applications cover compositions of matter and methods of use, which further strengthen Tempest’s intellectual property for the combined inhibition of EP2 and EP4 prostaglandin PGE2 receptor signaling.
About TPST-1495
TPST-1495 is an orally-available small molecule designed to block the EP2 and EP4 receptors in the prostaglandin (PGE2) pathway, while sparing the homologous but differentially active EP1 and EP3 receptors. PGE2 signaling through EP2 and EP4 has been observed both to enhance tumor progression and promote immune suppression. Tempest has conducted head-to-head preclinical studies comparing TPST-1495 to single antagonists of EP2 and EP4 and observed significantly enhanced activity of TPST-1495 in both overcoming PGE2-mediated suppression of human immune cells in vitro, as well as significantly increased anti-tumor activity in mouse models of human colorectal cancer. Tempest is currently evaluating the safety, tolerability, pharmacokinetics (PK), pharmacodynamics (PD), and possible anti-tumor activity of TPST-1495 in a multicenter Phase 1a/1b dose and schedule optimization study in subjects with advanced solid tumors, with the potential to expand in indications known to be prostaglandin-driven, including colorectal cancer, or CRC, and in a tumor indication-agnostic, biomarker-selected cohort.