Atrasentan

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Atrasentan
Clinical data
Trade namesVanrafia
Other namesABT-627, A-127722, atrasentan hydrochloride (USAN US)
License data
Pregnancy
category
  • Contraindicated
By mouth
Drug classEndothelin 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
JSmol)
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=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 checkY
  • Key:MOTJMGVDPWRKOC-QPVYNBJUSA-N checkY

  • 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
 ☒NcheckY (what is this?)  (verify)

Atrasentan, sold under the brand name Vanrafia, is a

by mouth.[1]

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

Medical uses

Atrasentan is

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. ^ a b c d e f g h https://www.accessdata.fda.gov/drugsatfda_docs/label/2025/219208s000lbl.pdf
  2. ^ a b c "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. 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. PMID 23871417
    .
  6. PMID 24722445
    .
  7. ^ Clinical trial number NCT01858532 for "Study Of Diabetic Nephropathy With Atrasentan (SONAR)" at ClinicalTrials.gov
  8. S2CID 113407761
    .
  9. 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. PMID 18316570
    .
  13. ^ "Atrasentan - Chinook Therapeutics". AdisInsight. Springer Nature Switzerland AG.


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