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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4716	943319-70-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ponatinib iclusig AP24534 ponatinib hydrochloride ponatinib HCl	a pan-Bcr-Abl protein kinase Inhibitor Molecular weight: 532.57 Formula: C29H27F3N6O CLOGP: 6.11 LIPINSKI: 2 HAC: 7 HDO: 1 TPSA: 65.77 ALOGS: -5.26 ROTB: 7 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ponatinib
iclusig
AP24534
ponatinib hydrochloride
ponatinib HCl

a pan-Bcr-Abl protein kinase Inhibitor

Molecular weight: 532.57
Formula: C29H27F3N6O
CLOGP: 6.11
LIPINSKI: 2
HAC: 7
HDO: 1
TPSA: 65.77
ALOGS: -5.26
ROTB: 7

Status: OFP

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

Drug dosage:

Dose	Unit	Route
45	mg	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Dec. 14, 2012	FDA	ARIAD

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
Acute lymphocytic leukaemia recurrent	264.55	21.94	59	6855	2210	63479898
Philadelphia chromosome positive	192.06	21.94	34	6880	372	63481736
Cytogenetic analysis abnormal	181.93	21.94	37	6877	883	63481225
Chronic myeloid leukaemia recurrent	153.65	21.94	26	6888	213	63481895
Blast crisis in myelogenous leukaemia	119.64	21.94	24	6890	533	63481575
Drug resistance	114.67	21.94	54	6860	22879	63459229
Death	111.85	21.94	168	6746	374213	63107895
Dry skin	103.80	21.94	69	6845	56818	63425290
Neoplasm progression	93.77	21.94	55	6859	36373	63445735
Blast cell crisis	87.88	21.94	14	6900	75	63482033

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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
Acute lymphocytic leukaemia recurrent	302.35	21.82	82	8715	2962	34945172
Drug resistance	193.81	21.82	105	8692	25822	34922312
Cytogenetic analysis abnormal	191.36	21.82	43	8754	696	34947438
Blast crisis in myelogenous leukaemia	183.15	21.82	40	8757	564	34947570
Neoplasm progression	164.81	21.82	91	8706	23209	34924925
Chronic myeloid leukaemia recurrent	136.00	21.82	26	8771	178	34947956
Philadelphia chromosome positive	125.79	21.82	27	8770	349	34947785
Death	101.59	21.82	272	8525	397777	34550357
Loss of therapeutic response	77.44	21.82	20	8777	594	34947540
Blast cell crisis	74.12	21.82	14	8783	89	34948045

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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
Acute lymphocytic leukaemia recurrent	395.56	18.80	100	11925	4624	79727739
Philadelphia chromosome positive	234.40	18.80	46	11979	644	79731719
Blast crisis in myelogenous leukaemia	223.61	18.80	46	11979	827	79731536
Drug resistance	210.27	18.80	110	11915	42103	79690260
Cytogenetic analysis abnormal	165.75	18.80	38	11987	1152	79731211
Neoplasm progression	150.67	18.80	95	11930	51587	79680776
Chronic myeloid leukaemia recurrent	145.20	18.80	27	11998	278	79732085
Death	132.26	18.80	274	11751	566240	79166123
Lipase increased	93.78	18.80	47	11978	16419	79715944
Peripheral arterial occlusive disease	93.20	18.80	38	11987	8220	79724143

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01EA05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS BCR-ABL tyrosine kinase inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000175076	Protein Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors

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

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Disease	Relation	SNOMED_ID	DOID
Chronic myeloid leukemia	indication	92818009	DOID:8552
Philadelphia chromosome-positive acute lymphoblastic leukemia	indication	425688002

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.98	acidic
pKa2	8.49	Basic
pKa3	5.58	Basic
pKa4	4.36	Basic

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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
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR THE TREATMENT OF LEUKEMIAS
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD OF TREATING CHRONIC MYELOGENOUS LEUKEMIA
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN

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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
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	Dec. 18, 2023	CHRONIC PHASE (CP) CHRONIC MYELOID LEUKEMIA (CML) WITH RESISTANCE OR INTOLERANCE TO AT LEAST TWO PRIOR KINASE INHIBITORS
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	Dec. 18, 2023	CHRONIC PHASE (CP) CHRONIC MYELOID LEUKEMIA (CML) WITH RESISTANCE OR INTOLERANCE TO AT LEAST TWO PRIOR KINASE INHIBITORS
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	Dec. 18, 2023	CHRONIC PHASE (CP) CHRONIC MYELOID LEUKEMIA (CML) WITH RESISTANCE OR INTOLERANCE TO AT LEAST TWO PRIOR KINASE INHIBITORS
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	Dec. 18, 2023	CHRONIC PHASE (CP) CHRONIC MYELOID LEUKEMIA (CML) WITH RESISTANCE OR INTOLERANCE TO AT LEAST TWO PRIOR KINASE INHIBITORS

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN	INHIBITOR	Kd	7.30	CHEMBL	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN	INHIBITOR	IC50	9.43	WOMBAT-PK	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		IC50	8.92	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	IC50	7.90	WOMBAT-PK
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		IC50	8.52	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	7.62	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	6.66	CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	7.44	CHEMBL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN		Kd	7.57	CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		Kd	5.92	CHEMBL

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External reference:

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ID	Source
0LI	PDB_CHEM_ID
014797	NDDF
014798	NDDF
1114544-31-8	SECONDARY_CAS_RN
1364347	RXNORM
196462	MMSL
24826799	PUBCHEM_CID
29016	MMSL
31534	MMSL
4032031	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-533	TABLET, FILM COATED	30 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-533	TABLET, FILM COATED	30 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-533	TABLET, FILM COATED	30 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-534	TABLET, FILM COATED	45 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-534	TABLET, FILM COATED	45 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-534	TABLET, FILM COATED	45 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-535	TABLET, FILM COATED	15 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-535	TABLET, FILM COATED	15 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-535	TABLET, FILM COATED	15 mg	ORAL	NDA	33 sections
Iclusig	HUMAN PRESCRIPTION DRUG LABEL	1	63020-536	TABLET, FILM COATED	10 mg	ORAL	NDA	33 sections

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