All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Molfile Inchi Smiles Synonyms: pralsetinib BLU-667 BLU123244 X581238 gavreto

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. Molecular weight: 533.61 Formula: C27H32FN9O2 CLOGP: 3.23 LIPINSKI: 2 HAC: 11 HDO: 3 TPSA: 135.53 ALOGS: -4.72 ROTB: 8 Status: ONP 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

avapritinibcabozantinibcapivasertibentrectinibgilteritiniblarotrectiniblenvatinibmidostaurinnintedanibpazopanibpexidartinibquizartinib show all 21 →

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	P07949	RET_HUMAN	INHIBITOR	IC50	9.39		SCIENTIFIC LITERATURE	DRUG LABEL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	IC50	7		DRUG LABEL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN	INHIBITOR	IC50	7.80		DRUG LABEL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN	INHIBITOR	IC50	8.66		DRUG LABEL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN	INHIBITOR	IC50	7.24		DRUG LABEL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	7.46		SCIENTIFIC LITERATURE
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR	IC50	7.96		DRUG LABEL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN	INHIBITOR	IC50	8.70		DRUG LABEL
NT-3 growth factor receptor	Kinase	Q16288	NTRK3_HUMAN	INHIBITOR	IC50	8.05		DRUG LABEL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN	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