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macimorelin 🐶 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 | 5271 | 381231-18-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Macimorelin stimulates GH release by activating growth hormone secretagogue receptors present in the pituitary and hypothalamus.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.389 | High | 0.82 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 14.622 | High | 0.82 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.573 | 10^-6 cm/s | High | 0.82 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.837 | uL/min/10^6 cells | High | 0.82 |
| dppb | Dog plasma protein binding (% unbound) | 20.410 | % | High | 0.82 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 27.040 | % | High | 0.82 |
| herg | hERG pIC50 | 4.439 | pIC50 | High | 0.82 |
| hh-clint | Human hepatocyte intrinsic clearance | 5.754 | uL/min/10^6 cells | High | 0.82 |
| hlm-clint | Human liver microsomal intrinsic clearance | 19.999 | uL/min/mg protein | High | 0.82 |
| hppb | Human plasma protein binding (% unbound) | 23.190 | % | High | 0.82 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,EPHB4,ERBB2,GRK2,ITK,MAPK10,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK | 21 | |||
| kinase-selectivity-class | PDK1 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 4.178 | High | 0.82 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 30.832 | High | 0.82 | |
| mppb | Mouse plasma protein binding (% unbound) | 13.460 | High | 0.82 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 7.482 | High | 0.82 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 25.610 | % | High | 0.82 |
| rh-clint | Rat hepatocyte intrinsic clearance | 21.330 | uL/min/10^6 cells | High | 0.82 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 59.610 | % | High | 0.82 |
| rppb | Rat plasma protein binding (% unbound) | 15.070 | % | High | 0.82 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 812.831 | uM | High | 0.82 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 11, 2019 | EMA | AETERNA ZENTARIS GMBH | |
| Dec. 20, 2017 | FDA | AETERNA ZENTARIS GMBH |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | V04CD06 | VARIOUS DIAGNOSTIC AGENTS OTHER DIAGNOSTIC AGENTS Tests for pituitary function |
| FDA EPC | N0000193785 | Growth Hormone Secretagogue Receptor Agonist |
| FDA MoA | N0000193786 | Growth Hormone Secretagogue Receptor Agonists |
Related Drugs by ATC class:
V04CD Tests for pituitary function 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Adult growth hormone deficiency | diagnosis | 421684006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.35 | acidic |
| pKa2 | 13.06 | acidic |
| pKa3 | 13.84 | acidic |
| pKa4 | 7.93 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 60MG BASE/POUCH | MACRILEN | AETERNA ZENTARIS | N205598 | Dec. 20, 2017 | DISCN | FOR SOLUTION | ORAL | 8192719 | Oct. 12, 2027 | A METHOD FOR THE DIAGNOSIS OF ADULT GROWTH HORMONE DEFICIENCY BY MEASURING THE LEVEL OF GROWTH HORMONE AFTER ORAL ADMINISTRATION OF MACIMORELIN |
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 | 7.81 | IUPHAR | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| 8680B21W73 | UNII |
| 945212-59-9 | SECONDARY_CAS_RN |
| 4037714 | VANDF |
| C2986922 | UMLSCUI |
| CHEBI:748011 | CHEBI |
| CHEMBL278623 | ChEMBL_ID |
| 9804938 | PUBCHEM_CID |
| DB13074 | DRUGBANK_ID |
| CHEMBL2364617 | ChEMBL_ID |
| D10563 | KEGG_DRUG |
| 9073 | INN_ID |
| C582727 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9745 | IUPHAR_LIGAND_ID |
| 781246008 | SNOMEDCT_US |
| 781266004 | SNOMEDCT_US |
| 33368 | MMSL |
| d08694 | MMSL |
| 017443 | NDDF |
| 017444 | NDDF |
| 1999419 | RXNORM |
| 8680B21W73 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Macrilen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0169-1401 | GRANULE, FOR SOLUTION | 60 mg | ORAL | NDA | 25 sections |
| Macrilen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 58844-130 | GRANULE, FOR SOLUTION | 60 mg | ORAL | NDA | 25 sections |