Atrasentan

Atrasentan, sold under the brand name Vanrafia, is a medication used to reduce proteinuria.^[1] It is an endothelin receptor antagonist.^[1] It is taken by mouth.^[1]

Atrasentan

Clinical data
Trade names	Vanrafia
Other names	ABT-627, A-127722, atrasentan hydrochloride (USAN US)
AHFS/Drugs.com	Monograph
MedlinePlus	a625070
License data	US DailyMed: Atrasentan
Pregnancy category	Contraindicated
Routes of administration	By mouth
Drug class	Endothelin receptor antagonist
ATC code	None
Legal status
Legal status	US: ℞-only[1]
Identifiers
IUPAC name (2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid
CAS Number	173937-91-2 N as HCl: 195733-43-8
PubChem CID	159594 as HCl: 159595
DrugBank	DB06199 as HCl: DBSALT001999
ChemSpider	140321 Y as HCl: 140322
UNII	V6D7VK2215 as HCl: E4G31X93ZA
KEGG	as HCl: D03009
ChEBI	CHEBI:135810
ChEMBL	ChEMBL9194 Y as HCl: ChEMBL2106068
ECHA InfoCard	100.206.784
Chemical and physical data
Formula	C29H38N2O6
Molar mass	510.631 g·mol−1
3D model (JSmol)	Interactive image as HCl: Interactive image
SMILES CCCCN(CCCC)C(=O)CN1C[C@@H]([C@H]([C@@H]1C2=CC=C(C=C2)OC)C(=O)O)C3=CC4=C(C=C3)OCO4 as HCl: Cl.CCCCN(CCCC)C(=O)CN1C[C@@H]([C@H]([C@@H]1C1=CC=C(OC)C=C1)C(O)=O)C1=CC=C2OCOC2=C1
InChI InChI=1S/C29H38N2O6/c1-4-6-14-30(15-7-5-2)26(32)18-31-17-23(21-10-13-24-25(16-21)37-19-36-24)27(29(33)34)28(31)20-8-11-22(35-3)12-9-20/h8-13,16,23,27-28H,4-7,14-15,17-19H2,1-3H3,(H,33,34)/t23-,27-,28+/m1/s1 Y Key:MOTJMGVDPWRKOC-QPVYNBJUSA-N Y as HCl: InChI=1S/C29H38N2O6.ClH/c1-4-6-14-30(15-7-5-2)26(32)18-31-17-23(21-10-13-24-25(16-21)37-19-36-24)27(29(33)34)28(31)20-8-11-22(35-3)12-9-20;/h8-13,16,23,27-28H,4-7,14-15,17-19H2,1-3H3,(H,33,34);1H/t23-,27-,28+;/m1./s1 Key:IJFUJIFSUKPWCZ-SQMFDTLJSA-N
NY (what is this?)  (verify)

Atrasentan was approved for medical use in the United States in April 2025.^[1][2]

Medical uses

Atrasentan is indicated to reduce proteinuria in adults with primary immunoglobulin A nephropathy at risk of rapid disease progression, generally a urine protein-to-creatinine ratio >= 1.5 g/g.^[1]

Society and culture

Legal status

Atrasentan was approved for medical use in the United States in April 2025.^[1][2]

Names

Atrasentan is the international nonproprietary name.^[3]

Atrasentan is sold under the brand name Vanrafia.^[1][2]

Research

Clinical trials

Atrasentan failed a phase III trial for prostate cancer in patients unresponsive to hormone therapy.^[4] A second trial confirmed this finding.^[5]

A study published in 2014 showed that 0.75 mg and 1.25 mg of atrasentan reduced urinary albumin by 35 and 38% respectively with modest side effects. Patients also had decreased home blood pressures (but no change in office readings) decrease total cholesterol and LDL. Patients in the 1.25 mg dose group had increased weight gain which was presumably due to increased edema and had to withdraw from the study more than the placebo or 0.75 mg dose group.^[6]

In 2013, the SONAR trial^[7] was initiated to determine if atrasentan reduces kidney failure in diabetic kidney disease.^[8]

In 2024, the phase III ALIGN trial found atrasentan to be effective in reducing proteinuria in participants with IgA nephropathy.^[9][10]

Atrasentan is being studied for the treatment of various types of cancer,^[11] including non-small-cell lung cancer.^[12] It is also being investigated as a therapy for diabetic kidney disease.^[13]