DB04894 - Vapreotide
| Identification | |
|---|---|
| Name | Vapreotide |
| Accession Number | DB04894 |
| Type | small molecule |
| Description | Vapreotide is a synthetic octapeptide somatostatin analog. It was being studied for the treatment of cancer. |
| Structure |
|
| Categories (*) | |
| Molecular Weight | 1131.371 |
| Groups | approved |
| Monoisotopic Weight | 1130.483013278 |
| Pharmacology | |
| Indication | For the treatment of esophageal variceal bleeding in patients with cirrhotic liver disease and has also shown efficacy in the treatment of patients with AIDS-related diarrhea. |
| Mechanism of action | The exact mechanism of action is unknown, although one study has provided in vitro and in vivo evidence for a tachykinin NK1 receptor antagonist effect in the analgesic effects of vapreotide (PMID: 7556407). |
| Absorption | Not Available |
| Protein binding | Not Available |
| Biotransformation | Not Available |
| Route of elimination | Vapreotide is 76% eliminated in bile. The remainder is renally eliminated. |
| Toxicity | Safety data are limited, however, headache, fatigue, diarrhea, nausea, vomiting, and abdominal pain have been reported commonly with the use of vapreotide. |
| Affected organisms |
|
| Interactions | |
| Drug Interactions | Not Available |
| Food Interactions | Not Available |
Targets
| Somatostatin receptor type 2 | |
|---|---|
| Name | Somatostatin receptor type 2 |
| Gene Name | SSTR2 |
| Pharmacological action | yes |
| Actions | inducer |
| References |
|
| DTHybrid score | 1.1089 |
| Somatostatin receptor type 5 | |
| Name | Somatostatin receptor type 5 |
| Gene Name | SSTR5 |
| Pharmacological action | yes |
| Actions | agonist |
| References |
|
| DTHybrid score | 1.1089 |
| Substance-P receptor | |
| Name | Substance-P receptor |
| Gene Name | TACR1 |
| Pharmacological action | unknown |
| Actions | antagonist |
| References |
|
| DTHybrid score | 0.5844 |
Predictions
| Id | Partner name | Gene Name | Score |
|---|---|---|---|
| 503 | Somatostatin receptor type 1 | SSTR1 | 0.5661 |
| 6009 | Somatostatin receptor type 3 | SSTR3 | 0.3335 |
| 1757 | Myeloperoxidase | MPO | 0.1323 |
| 4757 | Cytochrome P450 2C9 | CYP2C9 | 0.0382 |
| 4512 | Cytochrome P450 3A4 | CYP3A4 | 0.0336 |
| 706 | Glutamate [NMDA] receptor subunit 3A | GRIN3A | 0.0288 |
| 6107 | Cytochrome P450 3A7 | CYP3A7 | 0.0248 |
| 4118 | Cytochrome P450 3A5 | CYP3A5 | 0.0236 |
| 6016 | Cytochrome P450 2C19 | CYP2C19 | 0.0226 |
| 4200 | Cytochrome P450 1A2 | CYP1A2 | 0.0222 |
| 831 | D(2) dopamine receptor | DRD2 | 0.0222 |
| 20 | Prostaglandin G/H synthase 1 | PTGS1 | 0.0211 |
| 6030 | Cytochrome P450 2B6 | CYP2B6 | 0.0199 |
| 4924 | Cytochrome P450 2C8 | CYP2C8 | 0.0182 |
| 1588 | Multidrug resistance protein 1 | ABCB1 | 0.0166 |