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Details

Stereochemistry ABSOLUTE
Molecular Formula C29H38N2O6
Molecular Weight 510.6218
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ATRASENTAN

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

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

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

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
69.0 pM [Ki]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
89 ng/mL
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
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
4.12 ng/mL
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
1.72 ng/mL
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
242 ng/mL
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
358 ng/mL
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
489 ng/mL
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
819 ng/mL
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
544 ng/mL
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
62 ng/mL
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
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
580 ng × h/mL
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
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
13.07 ng × h/mL
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
5.31 ng × h/mL
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
1492 ng × h/mL
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
1591 ng × h/mL
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
2338 ng × h/mL
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
3162 ng × h/mL
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
5354 ng × h/mL
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
536 ng × h/mL
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
34.1 h
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
32 h
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
40.9 h
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
36.1 h
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
32.6 h
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
30 h
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
23.2 h
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
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1.2%
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 (unknown)
Highest studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
unhealthy
n = 9
Health Status: unhealthy
Condition: Refractory Malignancies
Sex: M+F
Food Status: UNKNOWN
Population Size: 9
Sources:
DLT: hyponatremia, hypotension...
Dose limiting toxicities:
hyponatremia (severe, 2 patients)
hypotension (serious, 1 pt)
Sources:
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Other AEs: low white blood count, Constipation...
Other AEs:
low white blood count (2 patients)
Constipation (1 pt)
Platelets decreased (1 pt)
Nausea (1 pt)
Arthralgia (1 pt)
glutamic pyruvic transaminase increase (1 pt)
Vomiting (1 pt)
absolute neutrophil count (1 pt)
Hypocalcemia (2 patients)
Weight gain (1 pt)
Dry mouth (1 pt)
Headache (2 patients)
Dyspnea (2 patients)
Allergic rhinitis (4 patients)
Edema (5 patients)
Fatigue (3 patients)
Sources:
0.75 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 0.75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.75 mg, 1 times / day
Sources:
unhealthy
n = 78
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 78
Sources:
Disc. AE: acute appendicitis, lung hemorrhage...
AEs leading to
discontinuation/dose reduction:
acute appendicitis (1 pt)
lung hemorrhage (1 pt)
fatigue (1 pt)
Peripheral edema (2 patients)
Sources:
1.25 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 1.25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1.25 mg, 1 times / day
Sources:
unhealthy
n = 83
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 83
Sources:
Disc. AE: Hypoglycemia, hyperkalemia...
Other AEs: Atheroma coronary artery...
AEs leading to
discontinuation/dose reduction:
Hypoglycemia (1 pt)
hyperkalemia (1 pt)
hyperkalemia (2 patients)
Other AEs:
Atheroma coronary artery (1 pt)
Sources:
90 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: multiple
Dose: 90 mg, 1 times / day
Sources:
unhealthy
n = 3
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 3
Sources:
DLT: peripheral edema, peripheral edema...
Dose limiting toxicities:
peripheral edema (grade 3, 1 pt)
peripheral edema (grade 3, 1 pt)
Sources:
AEs

AEs

AESignificanceDosePopulation
hypotension serious, 1 pt
DLT
75 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
unhealthy
n = 9
Health Status: unhealthy
Condition: Refractory Malignancies
Sex: M+F
Food Status: UNKNOWN
Population Size: 9
Sources:
hyponatremia severe, 2 patients
DLT
75 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
unhealthy
n = 9
Health Status: unhealthy
Condition: Refractory Malignancies
Sex: M+F
Food Status: UNKNOWN
Population Size: 9
Sources:
Arthralgia 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Constipation 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Dry mouth 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Nausea 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Platelets decreased 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Vomiting 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Weight gain 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
absolute neutrophil count 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
glutamic pyruvic transaminase increase 1 pt
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Dyspnea 2 patients
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Headache 2 patients
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Hypocalcemia 2 patients
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
low white blood count 2 patients
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Fatigue 3 patients
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Allergic rhinitis 4 patients
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
Edema 5 patients
70 mg 1 times / day multiple, oral (unknown)
MTD
Dose: 70 mg, 1 times / day
Route: oral
Route: multiple
Dose: 70 mg, 1 times / day
Sources:
unhealthy
n = 11
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 11
Sources:
acute appendicitis 1 pt
Disc. AE
0.75 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 0.75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.75 mg, 1 times / day
Sources:
unhealthy
n = 78
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 78
Sources:
fatigue 1 pt
Disc. AE
0.75 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 0.75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.75 mg, 1 times / day
Sources:
unhealthy
n = 78
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 78
Sources:
lung hemorrhage 1 pt
Disc. AE
0.75 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 0.75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.75 mg, 1 times / day
Sources:
unhealthy
n = 78
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 78
Sources:
Peripheral edema 2 patients
Disc. AE
0.75 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 0.75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 0.75 mg, 1 times / day
Sources:
unhealthy
n = 78
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 78
Sources:
Atheroma coronary artery 1 pt
1.25 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 1.25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1.25 mg, 1 times / day
Sources:
unhealthy
n = 83
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 83
Sources:
Hypoglycemia 1 pt
Disc. AE
1.25 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 1.25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1.25 mg, 1 times / day
Sources:
unhealthy
n = 83
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 83
Sources:
hyperkalemia 1 pt
Disc. AE
1.25 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 1.25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1.25 mg, 1 times / day
Sources:
unhealthy
n = 83
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 83
Sources:
hyperkalemia 2 patients
Disc. AE
1.25 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 1.25 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1.25 mg, 1 times / day
Sources:
unhealthy
n = 83
Health Status: unhealthy
Condition: diabetic neuropathy
Sex: M+F
Food Status: UNKNOWN
Population Size: 83
Sources:
peripheral edema grade 3, 1 pt
DLT
90 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: multiple
Dose: 90 mg, 1 times / day
Sources:
unhealthy
n = 3
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 3
Sources:
peripheral edema grade 3, 1 pt
DLT
90 mg 1 times / day multiple, oral (unknown)
Studied dose
Dose: 90 mg, 1 times / day
Route: oral
Route: multiple
Dose: 90 mg, 1 times / day
Sources:
unhealthy
n = 3
Health Status: unhealthy
Condition: malignant glioma
Sex: M+F
Food Status: UNKNOWN
Population Size: 3
Sources:
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Pharmacological characterization of A-127722: an orally active and highly potent ETA-selective receptor antagonist.
1996 Feb
2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
1996 Mar 1
Endothelins regulate mediator production of rat tissue-cultured mucosal mast cells. Up-regulation of Th1 and inhibition of Th2 cytokines.
2002 May
Therapeutic targeting of the endothelin a receptor in human nasopharyngeal carcinoma.
2006 Dec
Endothelin A receptor blockade reduces diabetic renal injury via an anti-inflammatory mechanism.
2007 Jan
Activation of the ET-1/ETA pathway contributes to erectile dysfunction associated with mineralocorticoid hypertension.
2008 Dec
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 Mar 1
Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography.
2011 Feb 24
Patents

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
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 Fri Dec 15 15:40:04 GMT 2023
Edited
by admin
on Fri Dec 15 15:40:04 GMT 2023
Record UNII
V6D7VK2215
Record Status Validated (UNII)
Record Version
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Name Type Language
ATRASENTAN
INN   MI   VANDF   WHO-DD  
INN  
Official Name English
atrasentan [INN]
Common Name English
(2R,3R,4S)-1-((DIBUTYLCARBAMOYL)METHYL)-2-(P-METHOXYPHENYL)-4-(3,4-(METHYLENEDIOXY)PHENYL)-3-PYRROLIDINECARBOXYLIC ACID
Common Name English
Atrasentan [WHO-DD]
Common Name English
ATRASENTAN [MI]
Common Name English
3-PYRROLIDINECARBOXYLIC ACID, 4-(1,3-BENZODIOXOL-5-YL)-1-(2-(DIBUTYLAMINO)-2-OXOETHYL)-2-(4-METHOXYPHENYL)-, (2R-(2.ALPHA.,3.BETA.,4.ALPHA.))
Common Name English
ATRASENTAN [VANDF]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 537116
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C61606
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
EVMPD
SUB20598
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
EPA CompTox
DTXSID40870204
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
FDA UNII
V6D7VK2215
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
SMS_ID
100000085968
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
MERCK INDEX
m2131
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY Merck Index
INN
7970
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
DRUG BANK
DB06199
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
CAS
173937-91-2
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
PUBCHEM
159594
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
WIKIPEDIA
ATRASENTAN
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
ChEMBL
CHEMBL9194
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
MESH
C430623
Created by admin on Fri Dec 15 15:40:04 GMT 2023 , Edited by admin on Fri Dec 15 15:40:04 GMT 2023
PRIMARY
Related Record Type Details
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SALT/SOLVATE -> PARENT
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ACTIVE MOIETY