Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C29H38N2O6 |
| Molecular Weight | 510.6218 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCN(CCCC)C(=O)CN1C[C@@H]([C@H]([C@@H]1C2=CC=C(OC)C=C2)C(O)=O)C3=CC=C4OCOC4=C3
InChI
InChIKey=MOTJMGVDPWRKOC-QPVYNBJUSA-N
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
| Molecular Formula | C29H38N2O6 |
| Molecular Weight | 510.6218 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/8632312
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/8632312
Atrasentan (ABT-627, A-127722) is a selective endothelin A receptor antagonist. Atrasentan is being developed by AbbVie as an oral treatment for diabetic nephropathies.Abbott Laboratories was conducting clinical development of atrasentan for the treatment of certain cancers, including phase II trials for prostate cancer. However, no recent development has been reported for cancer indications and development is presumed to be discontinued.
CNS Activity
Curator's Comment: No significant binding was observed in mouse brain or heart after intravenous injection of atrasentan (ABT-627, A-127722). However it was shown that the drug partially normalized the infarct volume and neurological deficit in animal models of cerebral ischemia and attenuated tactile allodynia in a diabetic rat model of neuropathic pain. In addition phase I safety study of atrasentan was conducted in adults with recurrent malignant glioma.
Originator
Approval Year
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
544 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
45 mg 1 times / day multiple, oral dose: 45 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
358 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
62 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
489 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
242 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
819 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
89 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
0.28 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21372210 |
0.25 mg single, oral dose: 0.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1.72 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21372210 |
0.75 mg single, oral dose: 0.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
4.12 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21372210 |
1.75 mg single, oral dose: 1.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5354 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
45 mg 1 times / day multiple, oral dose: 45 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1591 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
536 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
2338 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
1492 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
3162 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
580 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
0.71 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21372210 |
0.25 mg single, oral dose: 0.25 mg route of administration: Oral experiment type: SINGLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
5.31 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21372210 |
0.75 mg single, oral dose: 0.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
13.07 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/21372210 |
1.75 mg single, oral dose: 1.75 mg route of administration: Oral experiment type: SINGLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
30 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
45 mg 1 times / day multiple, oral dose: 45 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
40.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
23.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
36.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
32 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
30 mg 1 times / day multiple, oral dose: 30 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
32.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
60 mg 1 times / day multiple, oral dose: 60 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
|
34.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
5 mg 1 times / day multiple, oral dose: 5 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1.2% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/15240529 |
75 mg 1 times / day multiple, oral dose: 75 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
ATRASENTAN plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
75 mg 1 times / day multiple, oral Highest studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
DLT: hyponatremia, hypotension... Dose limiting toxicities: hyponatremia (severe, 2 patients) Sources: hypotension (serious, 1 pt) |
70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Other AEs: Nausea, Vomiting... Other AEs: Nausea (1 pt) Sources: Vomiting (1 pt) Weight gain (1 pt) absolute neutrophil count (1 pt) Hypocalcemia (2 patients) Platelets decreased (1 pt) glutamic pyruvic transaminase increase (1 pt) Arthralgia (1 pt) Constipation (1 pt) Headache (2 patients) low white blood count (2 patients) Dyspnea (2 patients) Dry mouth (1 pt) Allergic rhinitis (4 patients) Edema (5 patients) Fatigue (3 patients) |
0.75 mg 1 times / day multiple, oral Studied dose Dose: 0.75 mg, 1 times / day Route: oral Route: multiple Dose: 0.75 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: Peripheral edema, fatigue... AEs leading to discontinuation/dose reduction: Peripheral edema (2 patients) Sources: fatigue (1 pt) acute appendicitis (1 pt) lung hemorrhage (1 pt) |
1.25 mg 1 times / day multiple, oral Studied dose Dose: 1.25 mg, 1 times / day Route: oral Route: multiple Dose: 1.25 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
Disc. AE: hyperkalemia, hyperkalemia... Other AEs: Atheroma coronary artery... AEs leading to discontinuation/dose reduction: hyperkalemia (2 patients) Other AEs:hyperkalemia (1 pt) Hypoglycemia (1 pt) Atheroma coronary artery (1 pt) Sources: |
90 mg 1 times / day multiple, oral Studied dose Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
DLT: peripheral edema, peripheral edema... Dose limiting toxicities: peripheral edema (grade 3, 1 pt) Sources: peripheral edema (grade 3, 1 pt) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| hypotension | serious, 1 pt DLT |
75 mg 1 times / day multiple, oral Highest studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| hyponatremia | severe, 2 patients DLT |
75 mg 1 times / day multiple, oral Highest studied dose Dose: 75 mg, 1 times / day Route: oral Route: multiple Dose: 75 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Arthralgia | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Constipation | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Dry mouth | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Nausea | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Platelets decreased | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Vomiting | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Weight gain | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| absolute neutrophil count | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| glutamic pyruvic transaminase increase | 1 pt | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Dyspnea | 2 patients | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Headache | 2 patients | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Hypocalcemia | 2 patients | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| low white blood count | 2 patients | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Fatigue | 3 patients | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Allergic rhinitis | 4 patients | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Edema | 5 patients | 70 mg 1 times / day multiple, oral MTD Dose: 70 mg, 1 times / day Route: oral Route: multiple Dose: 70 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| acute appendicitis | 1 pt Disc. AE |
0.75 mg 1 times / day multiple, oral Studied dose Dose: 0.75 mg, 1 times / day Route: oral Route: multiple Dose: 0.75 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| fatigue | 1 pt Disc. AE |
0.75 mg 1 times / day multiple, oral Studied dose Dose: 0.75 mg, 1 times / day Route: oral Route: multiple Dose: 0.75 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| lung hemorrhage | 1 pt Disc. AE |
0.75 mg 1 times / day multiple, oral Studied dose Dose: 0.75 mg, 1 times / day Route: oral Route: multiple Dose: 0.75 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Peripheral edema | 2 patients Disc. AE |
0.75 mg 1 times / day multiple, oral Studied dose Dose: 0.75 mg, 1 times / day Route: oral Route: multiple Dose: 0.75 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Atheroma coronary artery | 1 pt | 1.25 mg 1 times / day multiple, oral Studied dose Dose: 1.25 mg, 1 times / day Route: oral Route: multiple Dose: 1.25 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| Hypoglycemia | 1 pt Disc. AE |
1.25 mg 1 times / day multiple, oral Studied dose Dose: 1.25 mg, 1 times / day Route: oral Route: multiple Dose: 1.25 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| hyperkalemia | 1 pt Disc. AE |
1.25 mg 1 times / day multiple, oral Studied dose Dose: 1.25 mg, 1 times / day Route: oral Route: multiple Dose: 1.25 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| hyperkalemia | 2 patients Disc. AE |
1.25 mg 1 times / day multiple, oral Studied dose Dose: 1.25 mg, 1 times / day Route: oral Route: multiple Dose: 1.25 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| peripheral edema | grade 3, 1 pt DLT |
90 mg 1 times / day multiple, oral Studied dose Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
| peripheral edema | grade 3, 1 pt DLT |
90 mg 1 times / day multiple, oral Studied dose Dose: 90 mg, 1 times / day Route: oral Route: multiple Dose: 90 mg, 1 times / day Sources: |
unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Celecoxib, but not indomethacin, ameliorates the hypertensive and perivascular fibrotic actions of cyclosporine in rats: role of endothelin signaling. | 2015-04-01 |
|
| Endothelin 1 activation of endothelin A receptor/NADPH oxidase pathway and diminished antioxidants critically contribute to endothelial progenitor cell reduction and dysfunction in salt-sensitive hypertension. | 2012-05 |
|
| Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography. | 2011-02-24 |
|
| Protective effects of angiotensin AT1 receptor blockade in malignant hypertension in the rat. | 2009-04-01 |
|
| Activation of the ET-1/ETA pathway contributes to erectile dysfunction associated with mineralocorticoid hypertension. | 2008-12 |
|
| DOCA-salt treatment enhances responses to endothelin-1 in murine corpus cavernosum. | 2008-06 |
|
| 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. | 2008-03-01 |
|
| Endothelin A receptor blockade reduces diabetic renal injury via an anti-inflammatory mechanism. | 2007-01 |
|
| Therapeutic targeting of the endothelin a receptor in human nasopharyngeal carcinoma. | 2006-12 |
|
| Endothelin receptor antagonists. | 2006-06 |
|
| Differential roles of peripheral and spinal endothelin receptors in the micturition reflex in rats. | 2004-10 |
|
| Endothelin receptors as novel targets in tumor therapy. | 2004-05-27 |
|
| Endothelin-1 increases vascular superoxide via endothelin(A)-NADPH oxidase pathway in low-renin hypertension. | 2003-02-25 |
|
| Effect of castration on endothelin receptors. | 2002-08 |
|
| ABT-627, a potent endothelin receptor A antagonist, inhibits ovarian carcinoma growth in vitro. | 2002-08 |
|
| Endothelins regulate mediator production of rat tissue-cultured mucosal mast cells. Up-regulation of Th1 and inhibition of Th2 cytokines. | 2002-05 |
|
| Endothelin and blood pressure regulation in the female rat: studies in normal pregnancy and with nitric oxide synthase inhibition-induced hypertension. | 2000 |
|
| 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. | 1996-03-01 |
|
| Endothelin-1 production and decreased endothelin B receptor expression in advanced prostate cancer. | 1996-02-15 |
|
| Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist. | 1996-02 |
Sample Use Guides
0.75, or 1.75 mg daily for 8 weeks atrasentan is generally safe and effective in reducing residual albuminuria and may ultimately improve renal outcomes in patients with type 2 diabetic nephropathy.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Apr 02 19:42:22 GMT 2025
by
admin
on
Wed Apr 02 19:42:22 GMT 2025
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| Record UNII |
P6FLG98GBJ
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| Record Status |
Validated (UNII)
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| Record Version |
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195704-72-4
Created by
admin on Wed Apr 02 19:42:22 GMT 2025 , Edited by admin on Wed Apr 02 19:42:22 GMT 2025
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P6FLG98GBJ
Created by
admin on Wed Apr 02 19:42:22 GMT 2025 , Edited by admin on Wed Apr 02 19:42:22 GMT 2025
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| Related Record | Type | Details | ||
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ENANTIOMER -> RACEMATE |
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ENANTIOMER -> RACEMATE |
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![Structure of 4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-3-pyrrolidinecarboxylic acid, (2S,3S,4R)-](/img/189e5b30-9122-414a-925e-b1de678f1727.svg "Structure of 4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-3-pyrrolidinecarboxylic acid, (2S,3S,4R)-")