U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry RACEMIC
Molecular Formula C29H38N2O6.ClH
Molecular Weight 547.083
Optical Activity ( + / - )
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of 4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-3-pyrrolidinecarboxylic acid hydrochloride, (2R,3R,4S)-rel-

SMILES

Cl.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=IJFUJIFSUKPWCZ-SQMFDTLJSA-N
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

HIDE SMILES / InChI
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
Molecular Formula ClH
Molecular Weight 36.461
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
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

CNS Non-penetrant
1040
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

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2849
 69.0 pM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase III
665
Unknown

Approved Use

Unknown
Primary
Phase III
665
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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

AUC

ValueDoseCo-administeredAnalytePopulation
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

T1/2

ValueDoseCo-administeredAnalytePopulation
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

Funbound

ValueDoseCo-administeredAnalytePopulation
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

Doses

DosePopulationAdverse 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:
https://pubmed.ncbi.nlm.nih.gov/15240529
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/15240529
DLT: hyponatremia, hypotension...
Dose limiting toxicities:
hyponatremia (severe, 2 patients)
hypotension (serious, 1 pt)
Sources:
https://pubmed.ncbi.nlm.nih.gov/15240529
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
Other AEs: Nausea, Vomiting...
Other AEs:
Nausea (1 pt)
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)
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
Disc. AE: Peripheral edema, fatigue...
AEs leading to
discontinuation/dose reduction:
Peripheral edema (2 patients)
fatigue (1 pt)
acute appendicitis (1 pt)
lung hemorrhage (1 pt)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
Disc. AE: hyperkalemia, hyperkalemia...
Other AEs: Atheroma coronary artery...
AEs leading to
discontinuation/dose reduction:
hyperkalemia (2 patients)
hyperkalemia (1 pt)
Hypoglycemia (1 pt)
Other AEs:
Atheroma coronary artery (1 pt)
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
DLT: peripheral edema, peripheral edema...
Dose limiting toxicities:
peripheral edema (grade 3, 1 pt)
peripheral edema (grade 3, 1 pt)
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
AEs

AEs

AESignificanceDosePopulation
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:
https://pubmed.ncbi.nlm.nih.gov/15240529
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/15240529
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:
https://pubmed.ncbi.nlm.nih.gov/15240529
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/15240529
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/24722445
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/24722445
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
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:
https://pubmed.ncbi.nlm.nih.gov/18477765
unhealthy
Health Status: unhealthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/18477765
Sourcing

Sourcing

Vendor/AggregatorIDURL
1PlusChem LLC
1P0038NU
https://www.1pchem.com/search?query=1P0038NU
AChemBlock
O32832
http://www.achemblock.com/catalogsearch/result/?q=O32832
Angene
AGN-PC-0WH6AV
http://www.angenechemical.com/productshow/AGN-PC-0WH6AV.html
BLD Pharm
BD630447
http://www.bldpharm.com/search/Search.html?keyword=BD630447
BOC Sciences
173937-91-2
http://www.bocsci.com/description.asp?cas=173937-91-2
BOC Sciences
195733-43-8
http://www.bocsci.com/description.asp?cas=195733-43-8
Chem Scene
CS-1373
http://www.chemscene.com/goproductList/searchProductList?productObj=CS-1373
ChemShuttle
178789
https://www.chemshuttle.com/catalogsearch/result/?q=178789
eMolecules
271447644
https://orderbb.emolecules.com/search/#?query=271447644
eMolecules
29917658
https://orderbb.emolecules.com/search/#?query=29917658
eMolecules
50282664
https://orderbb.emolecules.com/search/#?query=50282664
Hairui
ATXF025
http://www.hairuichem.com/en/product/search.do?q=ATXF025
mcule
MCULE-1574445963
https://mcule.com/MCULE-1574445963/
mcule
MCULE-4362237304
https://mcule.com/MCULE-4362237304/
mcule
MCULE-5848986494
https://mcule.com/MCULE-5848986494/
mcule
MCULE-6900549695
https://mcule.com/MCULE-6900549695/
MedChem Express
HY-15403A
https://www.medchemexpress.com/search.html?q=HY-15403A&ft=&fa=&fp=
MolPort
MolPort-044-724-665
https://www.molport.com/shop/molecule-link/MolPort-044-724-665
MuseChem
I002268
https://www.musechem.com/product/I002268.html
MuseChem
I003252
https://www.musechem.com/product/I003252.html
MuseChem
I014016
https://www.musechem.com/product/I014016.html
PI Chemicals
PI-41907
http://www.pipharm.com/catalog_products/PI-41907.html
Sigma Aldrich
SML2020
http://www.sigmaaldrich.com/catalog/search?term=SML2020&interface=All&N=0&mode=match%20partialmax&lang=en®ion=US&focus=product
Toronto Research Chemicals
A793925
https://www.trc-canada.com/product-detail/?CatNum=A793925
Toronto Research Chemicals
A793930
https://www.trc-canada.com/product-detail/?CatNum=A793930
PubMed

PubMed

TitleDatePubMed
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
Patents

Patents

US20160074363
4
US20160250186
4
WO/2015/038571A1
4

Sample Use Guides

In Vivo Use Guide
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
In Vitro Use Guide
Atrasentan (ABT-627, A-127722) exhibits a dose-dependent inhibition of ET-1-induced arachidonic acid release in human pericardium smooth muscle cells with a pA2 value of 10.5 and inhibits ET-1-induced vasoconstriction in isolated rat aorta with a pA2 value of 9.2.
Substance Class Chemical
Created
by admin
on Wed Apr 02 21:25:36 GMT 2025
Edited
by admin
on Wed Apr 02 21:25:36 GMT 2025
Record UNII
7D7JG7S7ZV
Record Status Validated (UNII)
Record Version
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Name Type Language
3-Pyrrolidinecarboxylic acid, 4-(1,3-benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-, hydrochloride (1:1), (2R,3R,4S)-rel-
Preferred Name English
4-(1,3-Benzodioxol-5-yl)-1-[2-(dibutylamino)-2-oxoethyl]-2-(4-methoxyphenyl)-3-pyrrolidinecarboxylic acid hydrochloride, (2R,3R,4S)-rel-
Systematic Name English
Code System Code Type Description
CAS
2984284-99-1
Created by admin on Wed Apr 02 21:25:36 GMT 2025 , Edited by admin on Wed Apr 02 21:25:36 GMT 2025
PRIMARY
FDA UNII
7D7JG7S7ZV
Created by admin on Wed Apr 02 21:25:36 GMT 2025 , Edited by admin on Wed Apr 02 21:25:36 GMT 2025
PRIMARY
Related Record Type Details
Structure of ATRASENTAN HYDROCHLORIDE
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