PF-610355
{{Drugbox | Watchedfields = changed | verifiedrevid = | IUPAC_name = N-[(4'-Hydroxy-3-biphenylyl)methyl]-2-[3-(2-{[(2R)-2-hydroxy-2-{4-hydroxy-3-[(methylsulfonyl)amino]phenyl}ethyl]amino}-2-methylpropyl)phenyl]acetamide | image = PF-610355.svg | width = 230
| tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | routes_of_administration = Inhalation | legal_status = Development terminated
| bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion =
| CAS_number = 862541-45-5
| ATC_prefix = None
| ATC_suffix =
| PubChem = 11505444
| IUPHAR_ligand =
| DrugBank_Ref = 
| DrugBank =
| ChemSpiderID_Ref =
| ChemSpiderID = 9680243
| UNII_Ref =
| UNII = ZH5SMU97AJ
| ChEMBL_Ref =
| ChEMBL = 1240967
| C = 34 | H = 39 | N = 3 | O = 6 | S = 1 | smiles = | StdInChI = | StdInChIKey = }}
PF-610355 (also known as PF-00610355 or PF-610,355) is an inhalable[1] ultra-long-acting β2 adrenoreceptor agonist[2] (ultra-LABA) that was investigated as a treatment of asthma and COPD by Pfizer.[3] It utilizes a sulfonamide agonist headgroup, that confers high levels of intrinsic crystallinity that could relate to the acidic sulfonamide motif supporting a zwitterionic form in the solid state. Optimization of pharmacokinetic properties minimized systemic exposure following inhalation and reduced systemically-mediated adverse events.[4] Its in vivo duration on action confirmed its potential for once-daily use in humans.[5]
The investigation and development of PF-610355 were discontinued in 2011,[6] likely for strategic and regulatory reasons.[7]
References
- ^ Diderichsen, Paul Matthias; Cox, Eugène; Martin, Steven W.; Cleton, Adriaan; Ribbing, Jakob (November 2013). "Predicted Heart Rate Effect of Inhaled PF-00610355, a Long Acting β-Adrenoceptor Agonist, in Volunteers and Patients With Chronic Obstructive Pulmonary Disease". British Journal of Clinical Pharmacology. 76 (5): 752–62. doi:10.1111/bcp.12080. PMC 3853534. PMID 23323609.
- ^ Cazzola, Mario; Luigino Calzetta; Maria Gabriella Matera3 (May 2011). "β2-adrenoceptor agonists: current and future direction". Br J Pharmacol. 163 (1): 4–17. doi:10.1111/j.1476-5381.2011.01216.x. PMC 3085864. PMID 21232045.
{{cite journal}}:|access-date=requires|url=(help)CS1 maint: numeric names: authors list (link) - ^ "Pfizer Pipeline as of January 27, 2010" (PDF). Pfizer Inc. p. 6. Retrieved 9 April 2016.
- ^ Glossop, PA; Lane, CA; Price, DA; Bunnage, ME; Lewthwaite, RA; James, K; Brown, AD; Yeadon, M; Perros-Huguet, C; Trevethick, MA; Clarke, NP; Webster, R; Jones, RM; Burrows, JL; Feeder, N; Taylor, SC; Spence, FJ (23 September 2010). "Inhalation by Design: Novel Ultra-Long-Acting β2-Adrenoreceptor Agonists for Inhaled Once-Daily Treatment of Asthma and Chronic Obstructive Pulmonary Disease That Utilize a Sulfonamide Agonist Headgroup". Journal of Medicinal Chemistry. 53 (18): 6640–52. doi:10.1021/jm1005989. PMID 20804199.
- ^ Acton, Q. Ashton (ed.). Issues in Medical Chemistry. 2011 Edition. ScholarlyEditions. ISBN 978-1-464-96440-4.
- ^ "AdisInsight: PF 610355". Springer International Publishing AG. Retrieved 25 March 2016.
- ^ Cazzola, M; Page, CP; Rogliani, P; Matera, MG (1 April 2013). "β2-Agonist Therapy in Lung Disease". American Journal of Respiratory and Critical Care Medicine. 187 (7): 693. doi:10.1164/rccm.201209-1739PP. PMID 23348973.
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