Atrasentan

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Atrasentan
Atrasentan structure.svg
Clinical data
Trade names Vanrafia
Other namesABT-627, A-127722, atrasentan hydrochloride (USAN US)
License data
Pregnancy
category
  • Contraindicated
Routes of
administration 		By mouth
Drug class Endothelin receptor antagonist
ATC code
  • None
Legal status
Legal status
Identifiers
  • (2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.206.784 OOjs UI icon edit-ltr-progressive.svg
Chemical and physical data
Formula C29H38N2O6
Molar mass 510.631 g·mol−1
3D model (JSmol)
  • 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=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 Yes check.svgY
  • Key:MOTJMGVDPWRKOC-QPVYNBJUSA-N Yes check.svgY

  • 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
 X mark.svgNYes check.svgY  (what is this?)    (verify)

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]

Contents

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

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]

References

  1. 1 2 3 4 5 6 7 8 https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/219208s000lbl.pdf
  2. 1 2 3 "Novartis receives FDA accelerated approval for Vanrafia (atrasentan), the first and only selective endothelin A receptor antagonist for proteinuria reduction in primary IgA nephropathy (IgAN)". Novartis (Press release). 3 April 2025. Retrieved 4 April 2025.
  3. ↑ World Health Organization (2001). "International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 46". WHO Drug Information. 15 (3–4): 187–218. hdl: 10665/71242 .
  4. ↑ "Addition of experimental drug to standard chemotherapy for advanced prostate cancer shows no benefit in phase 3 clinical trial" (Press release). National Cancer Institute. 21 April 2011. Retrieved 18 October 2014.
  5. ↑ Quinn DI, Tangen CM, Hussain M, Lara PN, Goldkorn A, Moinpour CM, et al. (August 2013). "Docetaxel and atrasentan versus docetaxel and placebo for men with advanced castration-resistant prostate cancer (SWOG S0421): a randomised phase 3 trial". The Lancet. Oncology. 14 (9): 893–900. doi:10.1016/S1470-2045(13)70294-8. PMC   4277263 . PMID   23871417.
  6. ↑ de Zeeuw D, Coll B, Andress D, Brennan JJ, Tang H, Houser M, et al. (May 2014). "The endothelin antagonist atrasentan lowers residual albuminuria in patients with type 2 diabetic nephropathy". Journal of the American Society of Nephrology. 25 (5): 1083–93. doi:10.1681/ASN.2013080830. PMC   4005314 . PMID   24722445.
  7. ↑ Clinical trial number NCT01858532 for "Study Of Diabetic Nephropathy With Atrasentan (SONAR)" at ClinicalTrials.gov
  8. ↑ Heerspink HJ, Parving HH, Andress DL, Bakris G, Correa-Rotter R, Hou FF, et al. (May 2019). "Atrasentan and renal events in patients with type 2 diabetes and chronic kidney disease (SONAR): a double-blind, randomised, placebo-controlled trial" (PDF). Lancet. 393 (10184): 1937–1947. doi:10.1016/S0140-6736(19)30772-X. PMID   30995972. S2CID   113407761.
  9. ↑ Heerspink HJ, Jardine M, Kohan DE, Lafayette RA, Levin A, Liew A, et al. (October 2024). "Atrasentan in Patients with IgA Nephropathy". The New England Journal of Medicine. doi:10.1056/NEJMoa2409415. PMID   39460694.
  10. ↑ "Novartis investigational atrasentan Phase III study demonstrates clinically meaningful and highly statistically significant proteinuria reduction in patients with IgA nephropathy (IgAN)". Novartis (Press release). 30 October 2023. Retrieved 4 April 2025.
  11. ↑ "NCI Drug Dictionary". National Cancer Institute. 2 February 2011. Retrieved 5 April 2025.
  12. ↑ Chiappori AA, Haura E, Rodriguez FA, Boulware D, Kapoor R, Neuger AM, et al. (March 2008). "Phase I/II study of atrasentan, an endothelin A receptor antagonist, in combination with paclitaxel and carboplatin as first-line therapy in advanced non-small cell lung cancer". Clinical Cancer Research. 14 (5): 1464–9. doi:10.1158/1078-0432.CCR-07-1508. PMID   18316570.
  13. ↑ "Atrasentan - Chinook Therapeutics". AdisInsight. Springer Nature Switzerland AG.


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