Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C16H20N4O2.ClH |
| Molecular Weight | 336.817 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CN1[C@H]2CC[C@@H]1C[C@@H](C2)NC(=O)N3C(=O)NC4=C3C=CC=C4
InChI
InChIKey=WKDOOXQPGYZUKZ-XSYYVRJTSA-N
InChI=1S/C16H20N4O2.ClH/c1-19-11-6-7-12(19)9-10(8-11)17-15(21)20-14-5-3-2-4-13(14)18-16(20)22;/h2-5,10-12H,6-9H2,1H3,(H,17,21)(H,18,22);1H/t10-,11+,12-;
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/8891590
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/8891590
DAU 6215 (Itasetron) is a selective 5-hydroxytryptamine3 (5-HT3) antagonist, which was developed by Boehringer Ingelheim. And was investigated for treatment the nausea and vomiting induced by chemotherapy, it was confirmed that this drug possessed antiemetic properties. Also was discovered, that chronic treatment with itasetron significantly improved retention abilities of the aged rats in this memory test. However, development of itasetron was terminated.
Approval Year
Doses
| Dose | Population | Adverse events |
|---|---|---|
8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Other AEs: Headache, Constipation... Other AEs: Headache Sources: Constipation Fatigue Anorexia bdominal pain |
280 ug/kg single, intravenous Highest studied dose Dose: 280 ug/kg Route: intravenous Route: single Dose: 280 ug/kg Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
Other AEs: Nausea, Dehydration... Other AEs: Nausea (grade 3, 14.3%) Sources: Dehydration (grade 3, 14.3%) Dry mouth (grade 1, 14.3%) Creatinine increased (grade 1-2) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Anorexia | 8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
| Constipation | 8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
| Fatigue | 8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
| Headache | 8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
| bdominal pain | 8 mg 2 times / day multiple, oral Highest studied dose Dose: 8 mg, 2 times / day Route: oral Route: multiple Dose: 8 mg, 2 times / day Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
|
| Dry mouth | grade 1, 14.3% | 280 ug/kg single, intravenous Highest studied dose Dose: 280 ug/kg Route: intravenous Route: single Dose: 280 ug/kg Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Creatinine increased | grade 1-2 | 280 ug/kg single, intravenous Highest studied dose Dose: 280 ug/kg Route: intravenous Route: single Dose: 280 ug/kg Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Dehydration | grade 3, 14.3% | 280 ug/kg single, intravenous Highest studied dose Dose: 280 ug/kg Route: intravenous Route: single Dose: 280 ug/kg Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
| Nausea | grade 3, 14.3% | 280 ug/kg single, intravenous Highest studied dose Dose: 280 ug/kg Route: intravenous Route: single Dose: 280 ug/kg Sources: |
unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Effect of DAU 6215, a novel 5-HT3 receptor antagonist, on scopolamine-induced amnesia in the rat in a spatial learning task. | 1994-01 |
|
| DAU 6215, a novel 5-HT3-receptor antagonist, selectively antagonizes scopolamine-induced deficit in a passive-avoidance task, but not scopolamine-induced hypermotility in rats. | 1993-09 |
Sample Use Guides
Nausea and vomiting: itasetron hydrochloride is effective in the dose range 35-280 microg/kg in preventing cisplatin-induced emesis.
Route of Administration:
Intravenous
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
127618-28-4
Created by
admin on Mon Mar 31 21:43:02 GMT 2025 , Edited by admin on Mon Mar 31 21:43:02 GMT 2025
|
PRIMARY | |||
|
m1199
Created by
admin on Mon Mar 31 21:43:02 GMT 2025 , Edited by admin on Mon Mar 31 21:43:02 GMT 2025
|
PRIMARY | Merck Index | ||
|
DTXSID30925919
Created by
admin on Mon Mar 31 21:43:02 GMT 2025 , Edited by admin on Mon Mar 31 21:43:02 GMT 2025
|
PRIMARY | |||
|
958C27ZK8Y
Created by
admin on Mon Mar 31 21:43:02 GMT 2025 , Edited by admin on Mon Mar 31 21:43:02 GMT 2025
|
PRIMARY |
ACTIVE MOIETY
SUBSTANCE RECORD
