Pavinetant

Pavinetant
Clinical data
Other names	MLE-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	941690-55-7;
PubChem CID	23649245;
ChemSpider	28189763;
UNII	3U471ZVC5K;
KEGG	D11345;
ChEBI	CHEBI:140478;
ChEMBL	ChEMBL3545233;
Chemical and physical data
Formula	C26H25N3O3S
Molar mass	459.564 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	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;

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]

References

http://adisinsight.springer.com/drugs/800038259
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.
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.
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.

External links

Pavinetant - AdisInsight

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[AdisInsight-1] ttp://adisinsight.springer.com/drugs/800038259

[pmid21417773-2] 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.

[pmid28385351-3] 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.

[pmid24525659-4] 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.

Neurokinin receptor modulators
NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96345 CP-99994 CP-122721 Dapitant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203040 GW-597599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67580 SDZ NKT 343 Serlopitant T-2328 Telmapitant Tradipitant Vestipitant Vofopitant
NK₂	Agonists: Neurokinin A Antagonists: GR-159897 Ibodutant Nepadutant Saredutant
NK₃	Agonists: Neurokinin B Senktide Antagonists: Fezolinetant (ESN-364) Osanetant (SR-142,801) Pavinetant (MLE-4901, AZD-2624, AZD-4901) SB-218,795 SB-222,200 Talnetant (SB-223,412)
See also: Receptor/signaling modulators • Signaling peptide/protein receptor modulators

Pavinetant

See also

References

External links