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Building the Next Generation of GPCR-Targeting Drugs

This article was originally published in Start Up

Executive Summary

One-third of marketed drugs hit G-protein coupled receptors, a group of cell-membrane bound receptors that are involved in almost every possible biological system. Drugs targeting GPCRs span most therapy areas, specialist or primary care, and may be small molecules, peptides, or large proteins. Despite their ubiquity, there's plenty of untapped potential too. Small wonder that start-ups continue to appear in this field, each with its own approach to improving existing drugs and finding new ones. We profile four in this issue.

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Receptos Inc.

Receptos isn't the only company in the G-coupled protein receptor oral MS drug arena, but it believes its proprietary S1P1 agonist will improve on Novartis' first-in-class S1P1 modulator Gilenya. Unlike Gilenya, which hits four of the five S1P receptor subtypes, the Receptos molecule binds selectively to S1P1 and has a predicted human half-life of approximately one day, potentially improving the safety profile and reducing complications for MS patients.

Receptos Inc.

Receptos isn't the only company in the G-coupled protein receptor oral MS drug arena, but it believes its proprietary S1P1 agonist will improve on Novartis' first-in-class S1P1 modulator Gilenya. Unlike Gilenya, which hits four of the five S1P receptor subtypes, the Receptos molecule binds selectively to S1P1 and has a predicted human half-life of approximately one day, potentially improving the safety profile and reducing complications for MS patients.

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