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- EP4 Antagonist
| Compound Code | RQ-0000007, RQ-00000008 |
|---|---|
| Primary Target Indications |
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| Development Stage | Phase 2a (chronic inflammatory pain) Phase 1 (acute pain) Pre-clinical trial (cancer) Portfolio for global development, manufacturing, and marketing rights |
| Product Summary | NSAIDs and COX-2 inhibitors relieve inflammation and pain by inhibiting the synthesis of prostaglandin E2 (PGE2). EP4, a PGE2 receptor, is associated with inflammatory pain. Selective EP4 receptor antagonists are different from NSAIDs and COX-2 inhibitors and do not inhibit arachidon acid cascade: since they directly block the action of PGE2, it is expected that they will not exhibit the side effects that NSAIDs and COX-2 inhibitors do. RQ-7 has completed Phase 2a for osteoarthritis, and we have confirmed that it has an equivalent effect on pain as NSAIDs. It has also been shown through endoscopic exams that it is safer for the gastrointestinal tract than NSAIDs. It is the world's first EP4 receptor antagonist that is useful for pain caused by osteoarthritis. RQ-8 has a different structure than RQ-7 and is a back-up compound with greater potency and selectivity than RQ-7. In addition to the effect on the inflammatory pain model, it has been confirmed that RQ-8 has a clear tumor-reducing effect in the occurrence of cancer pain. It has shown sufficient absorption and bioavailability in pharmacokinetic tests, and no problems have been observed yet in repeated-dose toxicity tests and genetic toxicity tests. |
| Non-Confidential Materials |
