CARA Therapeutics, Inc. is a clinical-stage biopharmaceutical company, which focuses on developing and commercializing new chemical entities designed to alleviate pruritus by selectively targeting peripheral kappa opioid receptors (KORs). Its portfolio includes opioid-based products, anesthetic-based drugs, and analgesics that targets to alleviate itch and pain. The company was founded by Derek T. Chalmers, Michael E. Lewis, and Frederique Menzaghi on July 2, 2004 and is headquartered in Stamford, CT.
Korsuva, is an analgesic opioid peptide used for the treatment of moderate to severe itching. It acts as a peripherally specific, highly selective agonist of the κ-opioid receptor (KOR).
Difelikefalin acts as an analgesic by activating KORs on peripheral nerve terminals and KORs expressed by certain immune system cells. Activation of KORs on peripheral nerve terminals results in the inhibition of ion channels responsible for afferent nerve activity, causing reduced transmission of pain signals, while activation of KORs expressed by immune system cells results in reduced release of proinflammatory, nerve-sensitizing mediators (e.g., prostaglandins).
Difelikefalin was approved for medical use in the United States in August 2021.The U.S. Food and Drug Administration considers it to be a first-in-class medication.
It is under development by Cara Therapeutics as an intravenous agent for the treatment of postoperative pain. An oral formulation has also been developed. Due to its peripheral selectivity, difelikefalin lacks the central side effects like sedation, dysphoria, and hallucinations of previous KOR-acting analgesics such as pentazocine and phenazocine.[8][9] In addition to use as an analgesic, difelikefalin is also being investigated for the treatment of pruritus (itching).Difelikefalin has completed phase II clinical trials for postoperative pain and has demonstrated significant and “robust” clinical efficacy, along with being safe and well tolerated. It has also completed a phase III clinical trial for uremic pruritus in hemodialysis patients.
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