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Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5379	1703793-34-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: avapritinib BLU-285 ayvakit	Avapritinib is a tyrosine kinase inhibitor that targets PDGFRA and PDGFRA D842 mutants as well as multiple KIT exon 11, 11/17 and 17 mutants with half maximal inhibitory concentrations (IC50s) less than 25 nM. Certain mutations in PDGFRA and KIT can result in the autophosphorylation and constitutive activation of these receptors which can contribute to tumor cell proliferation. Other potential targets for avapritinib include wild type KIT, PDGFRB, and CSFR1. Molecular weight: 498.57 Formula: C26H27FN10 CLOGP: 2.47 LIPINSKI: 0 HAC: 10 HDO: 1 TPSA: 106.29 ALOGS: -4.22 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

avapritinib
BLU-285
ayvakit

Avapritinib is a tyrosine kinase inhibitor that targets PDGFRA and PDGFRA D842 mutants as well as multiple KIT exon 11, 11/17 and 17 mutants with half maximal inhibitory concentrations (IC50s) less than 25 nM. Certain mutations in PDGFRA and KIT can result in the autophosphorylation and constitutive activation of these receptors which can contribute to tumor cell proliferation. Other potential targets for avapritinib include wild type KIT, PDGFRB, and CSFR1.

Molecular weight: 498.57
Formula: C26H27FN10
CLOGP: 2.47
LIPINSKI: 0
HAC: 10
HDO: 1
TPSA: 106.29
ALOGS: -4.22
ROTB: 5

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.30	g	O

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
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
azlogd74	LogD at pH 7.4	3.632		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	1.954		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	21.979	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	3.715	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	2.430	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	10.890	%	High	1
herg	hERG pIC50	5.393	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	2.600	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	9.441	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	1.760	%	High	1
kinase-safety-class	AAK1,ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB4,ERBB2,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,INSR,IRAK1,IRAK3,IRAK4,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK7,MARK3,MARK4,MELK,MET,MINK1,MKNK1,MKNK2,MST1R,NTRK1,NTRK2,NTRK3,NUAK1,PAK4,PDGFRB,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PRKAA1,PRKAA2,PRKCD,PRKDC,RET,RIPK3,ROCK1,ROCK2,RPS6KA1,SIK2,SIK3,SRC,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2,YES1	109
kinase-selectivity-class	ABL2,ACVR2B,ACVRL1,AKT3,AURKB,AURKC,AXL,BLK,BTK,CAMK2D,CHEK1,CLK2,CLK4,CSF1R,EGFR,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,IRAK3,KDR,KIT,LCK,LYN,MAP3K11,MAP3K7,MAP4K1,MAP4K3,MAP4K4,MAP4K5,MARK1,MARK2,MARK3,MARK4,MET,MINK1,MKNK2,NTRK1,NTRK3,NUAK1,PDGFRB,PDK1,RET,RIPK3,SIK2,SIK3,SRC,TGFBR1,TNIK,YES1	52
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	10.617		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	3.656		High	1
mppb	Mouse plasma protein binding (% unbound)	1.230		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	25.235		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pld-class	Phospholipidosis risk class (1 = positive, 0 = negative)	1		High	1
pppb	Pig plasma protein binding (% unbound)	3.650	%	High	1
rat-kpuu-brain	Rat brain Kpuu	0.042	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	5.957	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	12.010	%	High	1
rppb	Rat plasma protein binding (% unbound)	1.410	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	2.178	uM	High	1

Approvals:

Date	Agency	Company	Orphan
Sept. 24, 2020	EMA	Blueprint Medicines (Netherlands) B.V.
Jan. 9, 2020	FDA	BLUEPRINT MEDICINES

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
Off label use	147.26	31.12	138	1584	1102114	89524611
Periorbital oedema	101.69	31.12	24	1698	6775	90619950
Disease progression	86.25	31.12	47	1675	156568	90470157
Hair colour changes	77.42	31.12	17	1705	3477	90623248
Face oedema	76.44	31.12	25	1697	23293	90603432
Periorbital swelling	61.70	31.12	15	1707	4783	90621942
Tryptase increased	58.37	31.12	10	1712	557	90626168
Cognitive disorder	35.80	31.12	20	1702	69387	90557338
Persistent postural-perceptual dizziness	33.05	31.12	4	1718	16	90626709
Swelling face	32.85	31.12	20	1702	81332	90545393
Eye swelling	31.72	31.12	14	1708	29372	90597353

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
Off label use	145.65	38.89	134	1205	638201	41981795
Hair colour changes	105.02	38.89	22	1317	2180	42617816
Periorbital oedema	64.09	38.89	17	1322	4640	42615356
Memory impairment	45.86	38.89	25	1314	50197	42569799
Tryptase increased	45.22	38.89	8	1331	322	42619674
Face oedema	42.41	38.89	16	1323	13650	42606346

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
Off label use	162.78	29.87	178	2202	1500007	109086912
Hair colour changes	118.52	29.87	26	2354	4675	110582244
Face oedema	94.15	29.87	33	2347	33436	110553483
Periorbital oedema	89.02	29.87	24	2356	10168	110576751
Periorbital swelling	72.61	29.87	18	2362	5487	110581432
Disease progression	66.09	29.87	49	2331	243985	110342934
Tryptase increased	64.64	29.87	12	2368	931	110585988
Lacrimation increased	42.07	29.87	18	2362	30932	110555987
Eyelid oedema	38.90	29.87	14	2366	15248	110571671
Swelling face	37.89	29.87	24	2356	92297	110494622
Eye swelling	34.57	29.87	16	2364	33032	110553887
Nausea	34.20	29.87	79	2301	1235611	109351308
Memory impairment	33.09	29.87	30	2350	196914	110390005
Myelosuppression	32.54	29.87	22	2358	94318	110492601
Cognitive disorder	31.60	29.87	21	2359	87490	110499429

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EX18	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
FDA MoA	N0000020001	Tyrosine Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000185504	Cytochrome P450 2C9 Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA MoA	N0000191423	Multidrug and Toxin Extrusion Transporter 1 Inhibitors
FDA MoA	N0000193845	Bile Salt Export Pump Inhibitors
FDA MoA	N0000193932	Multidrug and Toxin Extrusion Transporter 2 K Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agent

Related Drugs by ATC class:

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Systemic mast cell disease	indication	397016004	DOID:349
Gastrointestinal stromal tumor	indication	420120006	DOID:9253

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.82	Basic
pKa2	6.22	Basic
pKa3	1.64	Basic
pKa4	1.05	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
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9200002	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9200002	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9944651	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9944651	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9994575	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9994575	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9200002	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9200002	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9944651	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9944651	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9994575	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9994575	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	11827642	Oct. 15, 2034	TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9200002	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9200002	Oct. 15, 2034	TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9944651	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9944651	Oct. 15, 2034	TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9994575	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9994575	Oct. 15, 2034	TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
300MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9200002	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
300MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9944651	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
300MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	9994575	Oct. 15, 2034	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
50MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9200002	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
50MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9944651	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
50MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	9994575	Oct. 15, 2034	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	11999744	April 10, 2040	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	11999744	April 10, 2040	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	11999744	April 10, 2040	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	11999744	April 10, 2040	TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	12252494	April 10, 2040	TREATMENT OF INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
50MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	11999744	April 10, 2040	TREATMENT OF ADVANCED SYSTEMIC MASTOCYTOSIS, INCLUDING PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	12060354	March 8, 2042	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	12060354	March 8, 2042	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION
300MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	12060354	March 8, 2042	TREATMENT OF UNRESECTABLE OR METASTATIC GASTROINTESTINAL STROMAL TUMOR (GIST) HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	May 22, 2026	TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	Jan. 9, 2027	INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	Jan. 9, 2027	INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	Jan. 9, 2027	INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS
300MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	Jan. 9, 2027	INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS
50MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	Jan. 9, 2027	INDICATED FOR THE TREATMENT OF ADULTS WITH UNRESECTABLE OR METASTATIC GIST HARBORING A PLATELET-DERIVED GROWTH FACTOR RECEPTOR ALPHA (PDGFRA) EXON 18 MUTATION, INCLUDING PDGFRA D842V MUTATIONS
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	June 16, 2028	FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	June 16, 2028	FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	June 16, 2028	FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
300MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	June 16, 2028	FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
50MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	June 16, 2028	FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED SYSTEMIC MASTOCYTOSIS (ADVSM). ADVSM INCLUDES PATIENTS WITH AGGRESSIVE SYSTEMIC MASTOCYTOSIS (ASM), SYSTEMIC MASTOCYTOSIS WITH AN ASSOCIATED HEMATOLOGICAL NEOPLASM (SM-AHN), AND MAST CELL LEUKEMIA (MCL)
100MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	May 22, 2030	TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
200MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	May 22, 2030	TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
25MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	May 22, 2030	TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
300MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	Jan. 9, 2020	RX	TABLET	ORAL	May 22, 2030	TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)
50MG	AYVAKIT	BLUEPRINT MEDICINES	N212608	June 16, 2021	RX	TABLET	ORAL	May 22, 2030	TREATMENT OF ADULT PATIENTS WITH INDOLENT SYSTEMIC MASTOCYTOSIS (ISM)

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	IC50	9.57	SCIENTIFIC LITERATURE	DRUG LABEL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN	INHIBITOR	IC50	9.62	SCIENTIFIC LITERATURE	DRUG LABEL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	8.82	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase		KIT_MOUSE	INHIBITOR	IC50	7.66	SCIENTIFIC LITERATURE

External reference:

ID	Source
513P80B4YJ	UNII
4039082	VANDF
C4743552	UMLSCUI
CHEBI:756628	CHEBI
9JI	PDB_CHEM_ID
CHEMBL4204794	ChEMBL_ID
118023034	PUBCHEM_CID
DB15233	DRUGBANK_ID
D000099289	MESH_DESCRIPTOR_UI
10613	INN_ID
D11279	KEGG_DRUG
10368	IUPHAR_LIGAND_ID
838409003	SNOMEDCT_US
838462005	SNOMEDCT_US
329235	MMSL
37922	MMSL
d09480	MMSL
018251	NDDF
2272107	RXNORM
513P80B4YJ	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ayvakit	HUMAN PRESCRIPTION DRUG LABEL	1	72064-110	TABLET, FILM COATED	100 mg	ORAL	NDA	31 sections
Ayvakit	HUMAN PRESCRIPTION DRUG LABEL	1	72064-120	TABLET, FILM COATED	200 mg	ORAL	NDA	31 sections
Ayvakit	HUMAN PRESCRIPTION DRUG LABEL	1	72064-125	TABLET, FILM COATED	25 mg	ORAL	NDA	31 sections
Ayvakit	HUMAN PRESCRIPTION DRUG LABEL	1	72064-130	TABLET, FILM COATED	300 mg	ORAL	NDA	31 sections
Ayvakit	HUMAN PRESCRIPTION DRUG LABEL	1	72064-150	TABLET, FILM COATED	50 mg	ORAL	NDA	31 sections

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avapritinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

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🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

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