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| Trade names | Korsuva |
| Other names | CR845, FE-202845, D-Phe-D-Phe-D-Leu-D-Lys-[γ-(4-N-piperidinyl)amino carboxylic acid][1] |
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| Routes of administration | Intravenous |
| Drug class | Kappa opioid receptor agonist |
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| Bioavailability | 100% (IV)[10] |
| Metabolism | Not metabolized[10] |
| Eliminationhalf-life | 2 hours[10] |
| Excretion | Excreted as unchanged drug viabile andurine[10] |
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| Chemical and physical data | |
| Formula | C36H53N7O6 |
| Molar mass | 679.863 g·mol−1 |
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Difelikefalin, sold under the brand nameKorsuva, is anopioid peptide used for the treatment of moderate to severeitch. It acts as aperipherally-restricted, highly selectiveagonist of theκ-opioid receptor (KOR).[10][11][12][13]
Difelikefalin acts as an analgesic by activating KORs on peripheralnerve terminals and KORs expressed by certainimmune systemcells.[10] Activation of KORs on peripheral nerve terminals results in the inhibition ofion channels responsible forafferentnerve activity, causing reduced transmission of pain signals, while activation of KORs expressed by immune system cells results in reduced release ofproinflammatory,nerve-sensitizing mediators (e.g.,prostaglandins).[10]
Difelikefalin was approved for medical use in the United States in August 2021.[8][14][15] The U.S.Food and Drug Administration considers it to be afirst-in-class medication.[16]
On 24 February 2022, theCommittee for Medicinal Products for Human Use (CHMP) of theEuropean Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Kapruvia, intended for treatment of moderate-to-severe pruritus associated with chronic kidney disease.[17] The applicant for this medicinal product is Vifor Fresenius Medical Care Renal Pharma France.[17] Difelikefalin was approved for medical use in the European Union in April 2022.[9][18]
It is under development byCara Therapeutics as anintravenous agent for the treatment ofpostoperative pain.[10][11][13] Anoral formulation has also been developed.[13] Due to its peripheral selectivity, difelikefalin lacks thecentralside effects likesedation,dysphoria, andhallucinations of previous KOR-acting analgesics such aspentazocine andphenazocine.[10][11] In addition to use as an analgesic, difelikefalin is also being investigated for the treatment ofpruritus (itching).[10][11][12] Difelikefalin has completedphase IIclinical trials for postoperative pain and has demonstrated significant and "robust" clinical efficacy, along with being safe and well tolerated.[11][13] It has also completed a phase III clinical trial foruremic pruritus inhemodialysis patients.[19]
This article incorporates text from this source, which is in thepublic domain.
