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anamorelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| growth hormone release-stimulating peptides | 5487 | 861998-00-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Anamorelin is a potent and selective novel ghrelin receptor agonist that mimics the N-terminal active core of ghrelin. ANAM stimulates neuroendocrine responses and can induce rapid positive effects on appetite and metabolism, which can lead to an increase in body weight and lean body mass.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.208 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 63.973 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.211 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 12.823 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 9.220 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 15.760 | % | High | 1 |
| herg | hERG pIC50 | 4.841 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 7.499 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 217.771 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 11.250 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,ERBB2,GRK2,ITK,MAPK10,MET,NTRK2,PDK1,PDK2,PDK4,PRKDC | 15 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 5.236 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 13.964 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 63.826 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 9.280 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 27.227 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 18.780 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.004 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 68.549 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 51.730 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 11.860 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 792.501 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 22, 2021 | PMDA | ONO PHARMACEUTICAL Co., Ltd |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Malignant neoplasm progression | 59.22 | 52.87 | 22 | 210 | 108378 | 42512725 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Malignant neoplasm progression | 104.84 | 41.59 | 35 | 398 | 174532 | 110414334 |
| Non-small cell lung cancer | 59.68 | 41.59 | 12 | 421 | 7923 | 110580943 |
| Interstitial lung disease | 42.33 | 41.59 | 17 | 416 | 139317 | 110449549 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Cancer cachexia | indication | 788876001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Growth hormone secretagogue receptor type 1 | GPCR | AGONIST | IC50 | 8.14 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 249921-19-5 | SECONDARY_CAS_RN |
| CHEBI:754417 | CHEBI |
| UYI | PDB_CHEM_ID |
| CHEMBL2110579 | ChEMBL_ID |
| C000593861 | MESH_SUPPLEMENTAL_RECORD_UI |
| 14127 | IUPHAR_LIGAND_ID |
| DB06645 | DRUGBANK_ID |
| D08856 | KEGG_DRUG |
| C2698934 | UMLSCUI |
| CHEMBL2103794 | ChEMBL_ID |
| 8846 | INN_ID |
| 9828911 | PUBCHEM_CID |
| 020167 | NDDF |
| DD5RBA1NKF | UNII |
| C524461 | MESH_SUPPLEMENTAL_RECORD_UI |
| DD5RBA1NKF | INXIGHT DRUGS |
Pharmaceutical products:
None