Atrasentan

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Atrasentan
Clinical data
ATC code
  • none
Identifiers
  • (2R,3R,4S)-4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)pyrrolidine-3-carboxylic acid
JSmol)
  • O=C(O)[C@H]4[C@H](c1ccc(OC)cc1)N(CC(=O)N(CCCC)CCCC)C[C@@H]4c2ccc3OCOc3c2
  • 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
 ☒NcheckY (what is this?)  (verify)

Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer,[1] including non-small cell lung cancer.[2] It is also being investigated as a therapy for diabetic kidney disease.

Atrasentan failed a phase 3 trial for prostate cancer in patients unresponsive to hormone therapy.[3] A second trial confirmed this finding.[4]

It is an

pulmonary arterial hypertension, atrasentan blocks endothelin induced cell proliferation.[citation needed
]

In April 2014, de Zeeuw et al. 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.[5] Reductions in proteinuria have been associated with beneficial patient outcomes in diabetic kidney disease with other interventions but is not an accepted end-point by the FDA.[citation needed]

In 2013, SONAR trial[6] was initiated to determine if atrasentan reduces kidney failure in diabetic kidney disease.[7]

References

  1. ^ "Atrasentan". NCI Dictionary of Cancer Terms. National Institute of Cancer. 2011-02-02.
  2. PMID 18316570
    .
  3. ^ "Addition of experimental drug to standard chemotherapy for advanced prostate cancer shows no benefit in phase 3 clinical trial" (Press release). National Cancer Institute. April 21, 2011. Retrieved October 18, 2014.
  4. PMID 23871417
    .
  5. PMID 24722445
    .
  6. ^ Clinical trial number NCT01858532 for "Study Of Diabetic Nephropathy With Atrasentan (SONAR)" at ClinicalTrials.gov
  7. S2CID 113407761
    .
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