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
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 |
DescriptionSources: http://adisinsight.springer.com/drugs/800008541Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/8632312
Sources: http://adisinsight.springer.com/drugs/800008541
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
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL252 Sources: https://www.ncbi.nlm.nih.gov/pubmed/8632312 |
69.0 pM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
|||
Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
|
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 |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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 |
|
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 |
|
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 |
|
32.6 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 |
|
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 |
|
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 |
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 (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) Sources: hypotension (serious, 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: |
Other AEs: low white blood count, Constipation... Other AEs: low white blood count (2 patients) Sources: 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) |
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) Sources: lung hemorrhage (1 pt) fatigue (1 pt) Peripheral edema (2 patients) |
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) Other AEs:hyperkalemia (1 pt) hyperkalemia (2 patients) 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) Sources: peripheral edema (grade 3, 1 pt) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
PubMed
Title | Date | PubMed |
---|---|---|
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 |
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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/8632312
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
Edited
Fri Dec 15 15:40:04 GMT 2023
by
admin
on
Fri Dec 15 15:40:04 GMT 2023
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Record UNII |
V6D7VK2215
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Record Status |
Validated (UNII)
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Record Version |
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FDA ORPHAN DRUG |
537116
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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
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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
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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
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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
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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
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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
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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
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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
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
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TRANSPORTER -> SUBSTRATE |
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TRANSPORTER -> SUBSTRATE |
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TRANSPORTER -> INHIBITOR |
Moderately inhibited P-gp in P388/dx cells.
IC50
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SALT/SOLVATE -> PARENT |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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