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ripretinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5394	1442472-39-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ripretinib qinlock DCC-2618	Ripretinib is a tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet derived growth factor receptor A (PDGFRA) kinase, including wild type, primary, and secondary mutations. Ripretinib also inhibits other kinases in vitro, such as PDGFRB, TIE2, VEGFR2, and BRAF Molecular weight: 510.37 Formula: C24H21BrFN5O2 CLOGP: 5.06 LIPINSKI: 1 HAC: 7 HDO: 3 TPSA: 86.36 ALOGS: -4.94 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ripretinib
qinlock
DCC-2618

Ripretinib is a tyrosine kinase inhibitor that inhibits KIT proto-oncogene receptor tyrosine kinase (KIT) and platelet derived growth factor receptor A (PDGFRA) kinase, including wild type, primary, and secondary mutations. Ripretinib also inhibits other kinases in vitro, such as PDGFRB, TIE2, VEGFR2, and BRAF

Molecular weight: 510.37
Formula: C24H21BrFN5O2
CLOGP: 5.06
LIPINSKI: 1
HAC: 7
HDO: 3
TPSA: 86.36
ALOGS: -4.94
ROTB: 5

Status: ONP

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

Drug dosage:

Dose	Unit	Route
0.15	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

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Date	Agency	Company	Orphan
May 15, 2020	FDA	DECIPHERA PHARMS
Nov. 18, 2021	EMA	DECIPHERA PHARMACEUTICALS (NETHERLANDS) B.V.

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FDA Adverse Event Reporting System (Female)

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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
Extra dose administered	133.90	37.04	30	1262	6320	63481410
Disease progression	131.31	37.04	59	1233	122699	63365031
Underdose	119.22	37.04	37	1255	27419	63460311
Palmar-plantar erythrodysaesthesia syndrome	75.14	37.04	25	1267	22990	63464740
Neoplasm progression	71.08	37.04	27	1265	36401	63451329
Alopecia	69.33	37.04	56	1236	337480	63150250
Hospitalisation	60.50	37.04	31	1261	85050	63402680
Death	46.75	37.04	47	1245	374334	63113396
Hyperkeratosis	43.20	37.04	12	1280	6006	63481724

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FDA Adverse Event Reporting System (Male)

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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
Extra dose administered	305.87	41.90	63	1547	3946	34951375
Disease progression	154.60	41.90	82	1528	107995	34847326
Alopecia	149.43	41.90	52	1558	24303	34931018
Fatigue	94.23	41.90	99	1511	370554	34584767
Underdose	86.58	41.90	30	1580	13750	34941571
Neoplasm progression	58.14	41.90	26	1584	23274	34932047
Hospitalisation	56.07	41.90	34	1576	56868	34898453
Hair texture abnormal	55.50	41.90	10	1600	302	34955019
Death	54.41	41.90	78	1532	397971	34557350
Adverse event	50.09	41.90	22	1588	18855	34936466

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FDA Adverse Event Reporting System (Geriatric)

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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
Extra dose administered	176.65	43.44	37	1074	8378	79734899
Alopecia	77.65	43.44	45	1066	231310	79511967
Fatigue	73.27	43.44	76	1035	929651	78813626
Underdose	71.53	43.44	24	1087	33127	79710150
Palmar-plantar erythrodysaesthesia syndrome	63.68	43.44	22	1089	33112	79710165
Death	62.69	43.44	56	1055	566458	79176819
Disease progression	56.84	43.44	34	1077	184328	79558949
Tumour excision	54.40	43.44	9	1102	557	79742720

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	L01EX19	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000020028	Platelet-derived Growth Factor alpha Receptor Inhibitors
FDA MoA	N0000020034	Stem Cell Factor (KIT) Receptor Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000187062	Cytochrome P450 2C8 Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Gastrointestinal stromal tumor	indication	420120006	DOID:9253

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	RE48731	June 7, 2032	TREATMENT OF GASTROINTESTINAL STROMAL TUMOR
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	10966966	Aug. 12, 2040	TREATMENT OF ADVANCED GASTROINTESTINAL STROMAL TUMOR IN PATIENTS HAVING PROGRESSED FROM A FIRST LINE ADMINISTRATION OF IMATINIB, A SECOND LINE ADMINISTRATION OF SUNITINIB, AND A THIRD LINE ADMINISTRATION OF REGORAFENIB
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	11266635	Aug. 12, 2040	TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM PALMER-PLANTER ERYTHRODYSESTHESIA SYNDROME
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	11344536	Aug. 12, 2040	TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM HYPERTENSION
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	11426390	Aug. 12, 2040	TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS BEING TREATED CONCURRENTLY WITH A CYP3A4 INHIBITOR
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	11433056	Aug. 12, 2040	METHOD OF TREATING GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM GRADE 2 OR GRADE 3 MYALGIA WHILE BEING ADMINISTERED RIPRETINIB DAILY
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	11529336	Aug. 12, 2040	TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM A GRADE 3 ADVERSE REACTION WHILE BEING ADMINISTERED RIPRETINIB DAILY
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	11534432	Aug. 12, 2040	TREATMENT OF ADVANCED GASTROINTESTINAL STROMAL TUMOR IN PATIENTS PREVIOUSLY ADMINISTERED AT LEAST THREE TYROSINE KINASE INHIBITORS, WHERE ONE OF THE KINASE INHIBITORS IS IMATINIB
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	11576904	Aug. 12, 2040	TREATMENT OF GASTROINTESTINAL STROMAL TUMORS IN PATIENTS SUFFERING FROM GRADE 2 OR GRADE 3 ARTHRALGIA WHILE BEING ADMINISTERED RIPRETINIB DAILY

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	May 15, 2025	NEW CHEMICAL ENTITY
50MG	QINLOCK	DECIPHERA PHARMS	N213973	May 15, 2020	RX	TABLET	ORAL	May 15, 2027	INDICATED FOR THE TREATMENT OF ADULT PATIENTS WITH ADVANCED GASTROINTESTINAL STROMAL TUMOR (GIST) WHO HAVE RECEIVED PRIOR TREATMENT WITH 3 OR MORE KINASE INHIBITORS, INCLUDING IMATINIB

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Bioactivity Summary:

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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	8.52	SCIENTIFIC LITERATURE	DRUG LABEL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN	INHIBITOR	IC50	8.44	SCIENTIFIC LITERATURE	DRUG LABEL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	IC50	8.05	DRUG LABEL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	8.47	DRUG LABEL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN	INHIBITOR	IC50	6.91	DRUG LABEL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN	INHIBITOR	IC50	8.27	DRUG LABEL

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External reference:

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ID	Source
018369	NDDF
10808	INN_ID
2369389	RXNORM
334366	MMSL
38467	MMSL
4039405	VANDF
71584930	PUBCHEM_CID
874906002	SNOMEDCT_US
876860008	SNOMEDCT_US
9175	IUPHAR_LIGAND_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
QINLOCK	HUMAN PRESCRIPTION DRUG LABEL	1	73207-101	TABLET	50 mg	ORAL	NDA	28 sections
QINLOCK	HUMAN PRESCRIPTION DRUG LABEL	1	73207-101	TABLET	50 mg	ORAL	NDA	28 sections
QINLOCK	HUMAN PRESCRIPTION DRUG LABEL	1	73207-101	TABLET	50 mg	ORAL	NDA	28 sections

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