Velufenacin

Velufenacin
Clinical data
Other names	DA-8010
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name [(3R)-1-Methylpyrrolidin-3-yl]methyl N-[2-(3-chloro-4-fluorophenyl)phenyl]carbamate;
CAS Number	1648737-78-3;
PubChem CID	121425461;
ChemSpider	88298721;
UNII	WV3E0S3IQB;
Chemical and physical data
Formula	C19H20ClFN2O2
Molar mass	362.83 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1CC[C@H](C1)COC(=O)NC2=CC=CC=C2C3=CC(=C(C=C3)F)Cl;
	InChI InChI=1S/C19H20ClFN2O2/c1-23-9-8-13(11-23)12-25-19(24)22-18-5-3-2-4-15(18)14-6-7-17(21)16(20)10-14/h2-7,10,13H,8-9,11-12H2,1H3,(H,22,24)/t13-/m1/s1; Key:SYBGVVSJNMTWCI-CYBMUJFWSA-N;

Velufenacin (DA-8010) is a muscarinic antagonist that operates on the M3 receptor and is tissue-selective for bladder over salivary glands. It is in development as a treatment for overactive bladder.^[1]^[2]^[3]^[4]

References

^ Son, Hee Seo; Oh, Cheol Young; Choo, Myung-Soo; Kim, Hyeong Gon; Kim, Joon Chul; Lee, Kyu-Sung; Shin, Dong Gil; Cho, Sung Yong; Jeong, Seong Jin; Seo, Ju Tae; Yoon, Hana; Moon, Hong Sang; Kim, Jang Hwan (June 2022). "Efficacy and Safety of DA-8010, a Novel M3 Antagonist, in Patients With Overactive Bladder: A Randomized, Double-Blind Phase 2 Study". International Neurourology Journal. 26 (2): 119–128. doi:10.5213/inj.2142382.191. ISSN 2093-4777. PMC 9260321. PMID 35793990.
^ Lee, Min Jung; Moon, Jun-Hwan; Lee, Hyung Keun; Cho, Chong Hwan; Choi, Sung Hak; Im, Weon-Bin (January 2019). "Pharmacological characterization of DA-8010, a novel muscarinic receptor antagonist selective for urinary bladder over salivary gland". European Journal of Pharmacology. 843: 240–250. doi:10.1016/j.ejphar.2018.11.037. PMID 30502343. S2CID 54471704.
^ Lee, Dae Young; Lee, Min Jung; Ryu, Chaelim; Lee, Heewon; Brooks, Ashley (February 2023). "Safety, tolerability, and pharmacokinetics of single and multiple ascending Oral doses of DA -8010 in healthy subjects: First-in-human phase I study". Pharmacology Research & Perspectives. 11 (1): e01040. doi:10.1002/prp2.1040. PMC 9897050. PMID 36734627.
^ Choi, Jin Bong; Jeon, Seung Hwan; Kwon, Eun Bi; Bae, Woong Jin; Cho, Hyuk Jin; Ha, U-Syn; Hong, Sung-Hoo; Lee, Ji Youl; Kim, Sae Woong (December 2020). "The effects of oral administration of the novel muscarinic receptor antagonist DA-8010 on overactive bladder in rat with bladder outlet obstruction". BMC Urology. 20 (1): 41. doi:10.1186/s12894-020-00611-8. PMC 7164290. PMID 32303205.

[1] Son, Hee Seo; Oh, Cheol Young; Choo, Myung-Soo; Kim, Hyeong Gon; Kim, Joon Chul; Lee, Kyu-Sung; Shin, Dong Gil; Cho, Sung Yong; Jeong, Seong Jin; Seo, Ju Tae; Yoon, Hana; Moon, Hong Sang; Kim, Jang Hwan (June 2022). "Efficacy and Safety of DA-8010, a Novel M3 Antagonist, in Patients With Overactive Bladder: A Randomized, Double-Blind Phase 2 Study". International Neurourology Journal. 26 (2): 119–128. doi:10.5213/inj.2142382.191. ISSN 2093-4777. PMC 9260321. PMID 35793990.

[2] Lee, Min Jung; Moon, Jun-Hwan; Lee, Hyung Keun; Cho, Chong Hwan; Choi, Sung Hak; Im, Weon-Bin (January 2019). "Pharmacological characterization of DA-8010, a novel muscarinic receptor antagonist selective for urinary bladder over salivary gland". European Journal of Pharmacology. 843: 240–250. doi:10.1016/j.ejphar.2018.11.037. PMID 30502343. S2CID 54471704.

[3] Lee, Dae Young; Lee, Min Jung; Ryu, Chaelim; Lee, Heewon; Brooks, Ashley (February 2023). "Safety, tolerability, and pharmacokinetics of single and multiple ascending Oral doses of DA -8010 in healthy subjects: First-in-human phase I study". Pharmacology Research & Perspectives. 11 (1): e01040. doi:10.1002/prp2.1040. PMC 9897050. PMID 36734627.

[4] Choi, Jin Bong; Jeon, Seung Hwan; Kwon, Eun Bi; Bae, Woong Jin; Cho, Hyuk Jin; Ha, U-Syn; Hong, Sung-Hoo; Lee, Ji Youl; Kim, Sae Woong (December 2020). "The effects of oral administration of the novel muscarinic receptor antagonist DA-8010 on overactive bladder in rat with bladder outlet obstruction". BMC Urology. 20 (1): 41. doi:10.1186/s12894-020-00611-8. PMC 7164290. PMID 32303205.

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