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pralsetinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| tyrosine kinase inhibitors | 5412 | 2097132-94-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Pralsetinib is a kinase inhibitor of wild-type RET and oncogenic RET fusions (CCDC6-RET) and mutations (RET V804L, RET V804M and RET M918T) with half maximal inhibitory concentrations (IC50s) less than 0.5 nM. In purified enzyme assays, pralsetinib inhibited DDR1, TRKC, FLT3, JAK1-2, TRKA, VEGFR2, PDGFRb, and FGFR1 at higher concentrations that were still clinically achievable at Cmax. In cellular assays, pralsetinib inhibited RET at approximately 14-, 40-, and 12-fold lower concentrations than VEGFR2, FGFR2, and JAK2, respectively.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ABL2,ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,GSK3B,HIPK2,IGF1R,IKBKB,INSR,IRAK1,IRAK3,ITK,JAK1,JAK2,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K2,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK15,MAPK7,MAPK9,MARK4,MELK,MET,MINK1,MST1R,NTRK1,NTRK2,NTRK3,NUAK1,PAK2,PAK4,PAK5,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CD,PIK3CG,PRKAA1,PRKAA2,PRKCD,PRKDC,RET,RIPK3,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2,YES1 | 124 | |||
| kinase-selectivity-class | ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BRAF,CAMK2B,CAMK2D,CDK1,CDK2,CDK9,CLK2,CLK4,CSF1R,DDR1,DYRK1B,EGFR,FGFR1,FLT3,IRAK1,JAK1,JAK2,KDR,KIT,LCK,MAP3K11,MAP3K21,MAP4K1,MAP4K3,MAPK7,MARK4,NTRK1,NTRK3,PDK1,PIK3CD,PRKCD,RET,SIK2,SIK3,STK33,SYK,TGFBR1,ULK1 | 45 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 4, 2020 | FDA | BLUEPRINT MEDICINES | |
| Nov. 18, 2021 | EMA | ROCHE REGISTRATION GMBH |
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 49.60 | 46.95 | 16 | 448 | 53575 | 90574408 |
| Disease progression | 48.82 | 46.95 | 21 | 443 | 156594 | 90471389 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Myelosuppression | 77.48 | 45.20 | 27 | 661 | 94313 | 110494298 |
| Disease progression | 74 | 45.20 | 34 | 654 | 244000 | 110344611 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01EX23 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors |
| MeSH PA | D000970 | Antineoplastic Agents |
| FDA EPC | N0000175605 | Kinase Inhibitor |
| FDA MoA | N0000193947 | Rearranged during Transfection (RET) Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
L01EX Other protein kinase inhibitors 21 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Non-small cell lung cancer | indication | 254637007 | DOID:3908 |
| Medullary thyroid carcinoma | indication | 255032005 | DOID:3973 |
| Metastatic non-small cell lung cancer | indication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | 10030005 | Nov. 1, 2036 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE) |
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | 10030005 | Nov. 1, 2036 | TREATMENT OF ADULT PATIENTS WITH METASTATIC REARRANGED DURING TRANSFECTION (RET) FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST |
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | 11273160 | April 3, 2039 | TREATMENT OF ADULT PATIENTS WITH METASTATIC REARRANGED DURING TRANSFECTION (RET) FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST |
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | 11872192 | April 3, 2039 | TREATMENT OF ADULT PATIENTS WITH METASTATIC REARRANGED DURING TRANSFECTION (RET) FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST |
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | 11963958 | April 3, 2039 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE) |
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | 12539303 | April 3, 2039 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE) |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | Sept. 4, 2027 | TREATMENT OF ADULT PATIENTS WITH METASTATIC RET FUSION-POSITIVE NON-SMALL CELL LUNG CANCER (NSCLC) AS DETECTED BY AN FDA APPROVED TEST |
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | Dec. 1, 2027 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET FUSION-POSITIVE THYROID CANCER WHO REQUIRE SYSTEMIC THERAPY AND WHO ARE RADIOACTIVE IODINE-REFRACTORY (IF RADIOACTIVE IODINE IS APPROPRIATE) |
| 100MG | GAVRETO | RIGEL PHARMS | N213721 | Sept. 4, 2020 | RX | CAPSULE | ORAL | Dec. 1, 2027 | TREATMENT OF ADULT AND PEDIATRIC PATIENTS 12 YEARS OF AGE AND OLDER WITH ADVANCED OR METASTATIC RET-MUTANT MEDULLARY THYROID CANCER (MTC) WHO REQUIRE SYSTEMIC THERAPY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Proto-oncogene tyrosine-protein kinase receptor Ret | Kinase | INHIBITOR | IC50 | 9.39 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Platelet-derived growth factor receptor beta | Kinase | INHIBITOR | IC50 | 7 | DRUG LABEL | ||||
| Receptor-type tyrosine-protein kinase FLT3 | Kinase | INHIBITOR | IC50 | 7.80 | DRUG LABEL | ||||
| Tyrosine-protein kinase JAK1 | Kinase | INHIBITOR | IC50 | 8.66 | DRUG LABEL | ||||
| High affinity nerve growth factor receptor | Kinase | INHIBITOR | IC50 | 7.24 | DRUG LABEL | ||||
| Vascular endothelial growth factor receptor 2 | Kinase | INHIBITOR | IC50 | 7.46 | SCIENTIFIC LITERATURE | ||||
| Fibroblast growth factor receptor 1 | Kinase | INHIBITOR | IC50 | 7.96 | DRUG LABEL | ||||
| Epithelial discoidin domain-containing receptor 1 | Kinase | INHIBITOR | IC50 | 8.70 | DRUG LABEL | ||||
| NT-3 growth factor receptor | Kinase | INHIBITOR | IC50 | 8.05 | DRUG LABEL | ||||
| Tyrosine-protein kinase JAK2 | Kinase | INHIBITOR | IC50 | 7.72 | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| D11712 | KEGG_DRUG |
| 1WPE73O1WV | UNII |
| C5226874 | UMLSCUI |
| CHEBI:757728 | CHEBI |
| Q4J | PDB_CHEM_ID |
| CHEMBL4582651 | ChEMBL_ID |
| 129073603 | PUBCHEM_CID |
| DB15822 | DRUGBANK_ID |
| 11004 | INN_ID |
| C000655704 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10033 | IUPHAR_LIGAND_ID |
| 926312002 | SNOMEDCT_US |
| 926317008 | SNOMEDCT_US |
| 4039706 | VANDF |
| 338525 | MMSL |
| 38786 | MMSL |
| d09624 | MMSL |
| 018493 | NDDF |
| 2394936 | RXNORM |
| 1WPE73O1WV | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Gavreto | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50242-210 | CAPSULE | 100 mg | ORAL | NDA | 31 sections |
| Gavreto | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71332-006 | CAPSULE | 100 mg | ORAL | NDA | 32 sections |