TPST-1495 is a dual antagonist of the prostaglandin E2 (PGE2) receptor subtypes EP2 and EP4, while sparing the immune-stimulating EP1 and EP3 receptors. TPST-1495 may help reduce the number of polyps in the small bowel and colon in patients with FAP.

2023年5月31日 · TPST-1495 is a novel oral therapy that inhibits signaling only at the tumor promoting EP2/EP4 receptors. In patients with heavily treated solid tumors, primarily MSS CRC, TPST-1495 had pharmacodynamic activity, a manageable safety profile, and a potential signal of activity consistent with the preclinical data and IO combination mechanism.

TPST-1495 is a dual antagonist of the prostaglandin E2 (PGE2) receptor subtypes EP2 and EP4, while sparing the immune-stimulating EP1 and EP3 receptors. TPST-1495 may help reduce the number of polyps in the small bowel and colon in patients with FAP.

Tempest has developed TPST 1495, a novel, highly selective and potent EP2-EP4 dual antagonist. In preclinical studies, TPST-1495 is significantly more potent than EP4-only antagonists. TPST-1495 effectively increases survival and modulates the TME in …

lung mets, 5 prior therapies in metastatic setting; TPST-1495 25 mgQD + pembrolizumab •Best overall response: SD (-22.5% tumor shrinkage) •Paired biopsies show high baseline COX-2 expression and increased CD8 + and CD8 + GrB + T

TPST-1495 (dual EP2/ep4 antagonist) A first-in-class oral antagonist selective for two receptors in the prostaglandin (PGE2) pathway, EP2 and EP4. COX-2 expression and increased prostaglandins synthesis are hallmarks of malignant tumor progression.

This is a first-in-human Phase 1a/1b, multicenter, open-label, dose-escalation, dose and schedule optimization, and expansion study of TPST-1495 as a single agent and in combination with pembrolizumab to determine its maximum tolerated dose (MTD) and or recommended Phase 2 dose (RP2D), safety, tolerability, pharmacokinetics, pharmacodynamics ...

TPST-1495 是一种口服的、高度特异性的 EP2 和 EP4 受体拮抗剂，不影响 EP1 和 EP3 受体以及 COX 酶。 临床前研究表明，与同时抑制所有 4 种受体、单独抑制 EP2 或 EP4 受体或抑制上游 COX-2 酶相比，用 TPST-1495 阻断 EP2 和 EP4 可更好地抑制肿瘤增殖并刺激抗癌免疫。 而通过 EP1 和 EP3 受体的信号传导通常是促炎的。 TPST-1495 是一种口服的、高度特异性的 EP2 和 EP4 受体拮抗剂，不影响 EP1 和 EP3 受体以及 COX 酶。

2025年3月13日 · About the TPST-1495 FAP Study . The planned Phase 2 study will evaluate the efficacy and safety of TPST-1495 in patients with Familial Adenomatous Polyposis (FAP) who have previously undergone ...

TPST-1495 binds to specific prostaglandin receptors specifically associated with tumor growth and suppression of the immune response. Giving TPST-1495 before surgery may help the immune system kill more tumor cells in patients with endometrial cancer or colorectal cancer.