Atrasentan

Structural formula
General
Non-proprietary name	Atrasentan
other names	(2 R , 3 R , 4 S ) -1 - [(Dibutylcarbamoyl) methyl] -2- ( p -methoxyphenyl) -4- [3,4- (methylenedioxy) phenyl] -3-pyrrolidinecarboxylic acid ( IUPAC )
Molecular formula	C 29 H 38 N 2 O 6
External identifiers / databases
CAS number 173937-91-2 EC number 681-642-4 ECHA InfoCard 100.206.784 PubChem 159594 ChemSpider 140321 DrugBank DB06199 Wikidata Q125083
Drug information
ATC code	L01 XX
Drug class	Cytostatic
properties
Molar mass	510.62 g · mol -1
safety instructions
Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed GHS labeling of hazardous substances danger H and P phrases H: 302-315-319-360 P: ?
As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Atrasentan (ABT-627) is an experimental drug being developed to treat prostate cancer and albuminuria associated with diabetic nephropathy .

The cytostatic effect of atrasentan comes about through its antagonistic binding to the endothelin -A receptor. Thereby it reduces cell proliferation and metastasis of tumor cells . Atrasentan is about to be launched in the United States as Xinlay ^® (manufacturer: Abbott ).

literature

Articles on analytics

• Bryan et al .: Determination of Atrasentan by high performance liquid chromatography with fluorescence detection in human plasma ., In: Biomed Chromatogr . , 15/8, 2001, pp. 525-533.
• Morley et al .: Determination of the endothelin receptor antagonist ABT-627 and related substances by high performance liquid chromatography , In: J Pharm Biomed Anal . , 7, 1999, pp. 777-784.

Articles on synthesis

• Boyd et al .: Discovery of a Series of Pyrrolidine-based Endothelin Receptor Antagonists with Enhanced ET _A Receptor Selectivity . In: Bio-Med-Chem. 7, 1999, pp. 991-1002.

Articles on pharmacology

• MA Carducci, A. Jimeno: Targeting bone metastasis in prostate cancer with endothelin receptor antagonists. In: Clin Cancer Res . 2006 Oct 15; 12 (20 Pt 2): 6296s-6300s, PMID 1706271 .
• Hammad et al .: Role of endothelin ET _A Receptor antagonism in the post-transplant renal response to angiotensin II in rats ., In: Exp. Physiol. , 83/3, 2001, 365-372.

Individual evidence

1. ↑ There is not yet a harmonized classification for this substance . A labeling of (2R, 3R, 4S) -4- (2H-1,3-benzodioxol-5-yl) -1 - [(dibutylcarbamoyl) methyl] -2- (4-methoxyphenyl) is shown, which is derived from a self-classification by the distributor ) pyrrolidine-3-carboxylic acid in the Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on December 17, 2019.
2. ↑ Clinical Study (Phase II): Evaluate the Efficacy and Safety of Once Daily Administration of Atrasentan Tablets (Low and High) Compared to Placebo in Reducing Residual Albuminuria in Type 2 Diabetic Patients With Nephropathy Who Are Treated With the Maximum Tolerated Labeled Dose of a Renin Angiotensin System (RAS) Inhibitor (RADAR) at Clinicaltrials.gov of the NIH
3. ↑ Clinical Study (Phase II): A Study of Atrasentan on Reducing Albuminuria in Type 2 Diabetic Nephropathy Treated With Renin-Angiotensin System Inhibitors at Clinicaltrials.gov of the NIH
4. ↑ ABDA database (as of December 4, 2009).

This article is about a health issue. It is not used for self-diagnosis and does not replace a diagnosis by a doctor. Please note the information on health issues !