Chemistry:PF-610355
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| Routes of administration | Inhalation |
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| Formula | C34H39N3O6S |
| Molar mass | 617.76 g·mol−1 |
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
- ↑ "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. November 2013. doi:10.1111/bcp.12080. PMID 23323609.
- ↑ "β(2) -adrenoceptor agonists: current and future direction". British Journal of Pharmacology 163 (1): 4–17. May 2011. doi:10.1111/j.1476-5381.2011.01216.x. PMID 21232045.
- ↑ "Pfizer Pipeline as of January 27, 2010". Pfizer Inc.. p. 6. http://www.pfizer.com/sites/default/files/product-pipeline/FINAL_27Jan10_Disclosed%20Portfolio.pdf.
- ↑ "Inhalation by design: novel ultra-long-acting β(2)-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. September 2010. doi:10.1021/jm1005989. PMID 20804199.
- ↑ Acton, Q. Ashton, ed (2012-01-09). Issues in Medical Chemistry Edition. ScholarlyEditions. ISBN 978-1-464-96440-4.
- ↑ "AdisInsight: PF 610355". Springer International Publishing AG. http://adisinsight.springer.com/drugs/800025582.
- ↑ "β2-agonist therapy in lung disease". American Journal of Respiratory and Critical Care Medicine 187 (7): 690–6. April 2013. doi:10.1164/rccm.201209-1739PP. PMID 23348973.
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