Pavinetant

Pavinetant (INN, USAN; developmental code names MLE-4901, AZD-4901, AZ-12472520, AZD-2624), is a small-molecule, orally active, selective neurokinin-3 (NK3) receptor antagonist which was under development by AstraZeneca and Millendo Therapeutics for the treatment of hot flashes and polycystic ovary syndrome (PCOS).[1][2][3] It was also under investigation for the treatment of schizophrenia,[2] but development was discontinued for this indication due to lack of effectiveness.[1][4] In November 2017, development of the medication for hot flashes and PCOS was also terminated after its developer assessed the clinical risks and benefits.[1][3]

Pavinetant
Clinical data
Other namesMLE-4901; AZD-4901; AZD-2624; AZ-12472520
Routes of
administration		By mouth
Identifiers
IUPAC name
  • 3-(methanesulfonamido)-2-phenyl-N-[(1S)-1-phenylpropyl]quinoline-4-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H25N3O3S
Molar mass459.56 g·mol−1
3D model (JSmol)
SMILES
  • CC[C@@H](C1=CC=CC=C1)NC(=O)C2=C(C(=NC3=CC=CC=C32)C4=CC=CC=C4)NS(=O)(=O)C
InChI
  • InChI=1S/C26H25N3O3S/c1-3-21(18-12-6-4-7-13-18)28-26(30)23-20-16-10-11-17-22(20)27-24(19-14-8-5-9-15-19)25(23)29-33(2,31)32/h4-17,21,29H,3H2,1-2H3,(H,28,30)/t21-/m0/s1
  • Key:QYTBBBAHNIWFOD-NRFANRHFSA-N

See also
  • Tachykinin receptor 3 § Agonists

References
  1. "Pavinetant - Millendo Therapeutics - AdisInsight".
  2. Malherbe P, Ballard TM, Ratni H (2011). "Tachykinin neurokinin 3 receptor antagonists: a patent review (2005 - 2010)". Expert Opin Ther Pat. 21 (5): 637–55. doi:10.1517/13543776.2011.568482. PMID 21417773. S2CID 207473995.
  3. Sassarini J, Anderson RA (2017). "New pathways in the treatment for menopausal hot flushes". Lancet. 389 (10081): 1775–1777. doi:10.1016/S0140-6736(17)30886-3. PMID 28385351.
  4. Litman RE, Smith MA, Desai DG, Simpson T, Sweitzer D, Kanes SJ (2014). "The selective neurokinin 3 antagonist AZD2624 does not improve symptoms or cognition in schizophrenia: a proof-of-principle study". J Clin Psychopharmacol. 34 (2): 199–204. doi:10.1097/JCP.0000000000000071. PMID 24525659. S2CID 33936765.



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