glasdegib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| SMO receptor antagonists | 5304 | 1095173-27-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Glasdegib is an inhibitor of the Hedgehog pathway. Glasdegib binds to and inhibits Smoothened, a transmembrane protein involved in hedgehog signal transduction.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 21, 2018 | FDA | PFIZER INC |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Febrile neutropenia | 108.54 | 51.72 | 32 | 199 | 118417 | 63370374 |
| Death | 59.62 | 51.72 | 28 | 203 | 374353 | 63114438 |
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 |
|---|---|---|---|---|---|---|
| Febrile neutropenia | 93.57 | 48.75 | 38 | 295 | 136811 | 34819787 |
| Pneumonia | 53.50 | 48.75 | 36 | 297 | 362591 | 34594007 |
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 |
|---|---|---|---|---|---|---|
| Febrile neutropenia | 193.17 | 47.27 | 70 | 541 | 230929 | 79512848 |
| Death | 88.56 | 47.27 | 54 | 557 | 566460 | 79177317 |
| Pneumonia | 53.10 | 47.27 | 42 | 569 | 660204 | 79083573 |
| Neoplasm progression | 47.54 | 47.27 | 17 | 594 | 51665 | 79692112 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XJ03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Hedgehog pathway inhibitors |
| FDA MoA | N0000184148 | Smoothened Receptor Antagonists |
| FDA EPC | N0000184149 | Hedgehog Pathway Inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:66908 | SMO receptor antagonists |
| CHEBI has role | CHEBI:140921 | Hedgehog pathway inhibitors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Acute myeloid leukemia, disease | indication | 91861009 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.45 | acidic |
| pKa2 | 12.88 | acidic |
| pKa3 | 13.49 | acidic |
| pKa4 | 7.85 | Basic |
| pKa5 | 6.86 | 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 25MG BASE | DAURISMO | PFIZER | N210656 | Nov. 21, 2018 | RX | TABLET | ORAL | 11168066 | April 13, 2036 | USE, IN COMBINATION WITH LOW-DOSE CYTARABINE, FOR THE TREATMENT OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) IN ADULT PATIENTS WHO ARE >= 75 YEARS OLD OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 25MG BASE | DAURISMO | PFIZER | N210656 | Nov. 21, 2018 | RX | TABLET | ORAL | Nov. 21, 2023 | NEW CHEMICAL ENTITY |
| EQ 25MG BASE | DAURISMO | PFIZER | N210656 | Nov. 21, 2018 | RX | TABLET | ORAL | Nov. 21, 2025 | INDICATED, IN COMBINATION WITH LOW-DOSE CYTARABINE, FOR THE TREATMENT OF NEWLY-DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) IN ADULT PATIENTS WHO ARE >=75 YEARS OLD OR WHO HAVE COMORBIDITIES THAT PRECLUDE USE OF INTENSIVE INDUCTION CHEMOTHERAPY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Smoothened homolog | GPCR | ANTAGONIST | IC50 | 8.30 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Smoothened homolog | GPCR | IC50 | 8.30 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| K673DMO5H9 | UNII |
| C4519273 | UMLSCUI |
| CHEBI:145428 | CHEBI |
| CHEMBL2043437 | ChEMBL_ID |
| 25166913 | PUBCHEM_CID |
| DB11978 | DRUGBANK_ID |
| CHEMBL4297534 | ChEMBL_ID |
| D10636 | KEGG_DRUG |
| 9930 | INN_ID |
| 8201 | IUPHAR_LIGAND_ID |
| 017851 | NDDF |
| 782978008 | SNOMEDCT_US |
| 783019002 | SNOMEDCT_US |
| 4038031 | VANDF |
| 2105845 | RXNORM |
| 299196 | MMSL |
| d09075 | MMSL |
| C000592580 | MESH_SUPPLEMENTAL_RECORD_UI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Daurismo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-0298 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 31 sections |
| Daurismo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-0298 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 31 sections |
| Daurismo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-1531 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 31 sections |
| Daurismo | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-1531 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 31 sections |