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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: ONP 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: ONP

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

Drug dosage:

Dose	Unit	Route
45	mg	O

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	4.474		Moderate	0.72
caco2-efflux	Caco-2 efflux ratio (BA/AB)	4.446		Moderate	0.72
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	4.150	10^-6 cm/s	Moderate	0.72
dh-clint	Dog hepatocyte intrinsic clearance	12.589	uL/min/10^6 cells	Moderate	0.72
dppb	Dog plasma protein binding (% unbound)	0.610	%	Moderate	0.72
fcs-ppb	Fetal calf serum protein binding (% unbound)	3.100	%	Moderate	0.72
herg	hERG pIC50	5.293	pIC50	Moderate	0.72
hh-clint	Human hepatocyte intrinsic clearance	3.027	uL/min/10^6 cells	Moderate	0.72
hlm-clint	Human liver microsomal intrinsic clearance	18.707	uL/min/mg protein	Moderate	0.72
hppb	Human plasma protein binding (% unbound)	0.480	%	Moderate	0.72
kinase-safety-class	ABL1,ABL2,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK1,CDK19,CDK5,CDK9,CHEK1,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB1,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,IKBKB,INSR,IRAK1,IRAK3,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK11,MAPK14,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK4,MELK,MET,MINK1,MKNK2,MST1R,MTOR,NTRK1,NTRK2,NTRK3,PAK4,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,PTK6,RET,RIPK3,RPS6KA1,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,ULK1,ULK2,YES1	110
kinase-selectivity-class	ABL2,ALK,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2D,CDK4,CDK7,CDK8,CDK9,CSF1R,CSK,DDR1,EGFR,EIF2AK3,EPHA2,EPHB3,EPHB4,ERBB2,ERBB4,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,IGF1R,INSR,IRAK1,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP2K1,MAP3K11,MAP3K2,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK11,MAPK12,MAPK14,MAPK7,MARK4,MET,MINK1,MKNK2,MST1R,MTOR,NTRK1,NTRK3,PAK4,PDGFRB,PDK1,PDK4,PIK3CA,PIK3CD,PRKCD,PRKDC,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK33,STK4,SYK,TEK,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1	85
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	10.889		Moderate	0.72
mh-clint	Mouse hepatocyte intrinsic clearance	19.679		Moderate	0.72
mppb	Mouse plasma protein binding (% unbound)	0.400		Moderate	0.72
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	23.281		Moderate	0.72
pfas-class	PFAS structural alert (1 = True, 0 = False)	1
pppb	Pig plasma protein binding (% unbound)	1.330	%	Moderate	0.72
rh-clint	Rat hepatocyte intrinsic clearance	20.091	uL/min/10^6 cells	Moderate	0.72
rh-fuinc	Rat hepatocyte fraction unbound in incubation	1.900	%	Moderate	0.72
rppb	Rat plasma protein binding (% unbound)	0.450	%	Moderate	0.72
solubility-dd	Solubility at pH 7.4 in DMSO	1.161	uM	Moderate	0.72

Approvals:

Date	Agency	Company	Orphan
Dec. 14, 2012	FDA	ARIAD

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
Acute lymphocytic leukaemia recurrent	348.43	21.67	74	8167	2647	90617559
Cytogenetic analysis abnormal	221.61	21.67	43	8198	967	90619239
Philadelphia chromosome positive	198.44	21.67	35	8206	455	90619751
Death	186.97	21.67	218	8023	456333	90163873
Blast crisis in myelogenous leukaemia	169.00	21.67	32	8209	629	90619577
Drug resistance	168.93	21.67	73	8168	30376	90589830
Chronic myeloid leukaemia recurrent	159.12	21.67	27	8214	275	90619931
Cytopenia	117.38	21.67	48	8193	17401	90602805
Thrombocytopenia	95.77	21.67	106	8135	208619	90411587
Neoplasm progression	95.37	21.67	56	8185	44430	90575776
Dry skin	90.00	21.67	70	8171	88003	90532203
Central nervous system leukaemia	88.88	21.67	16	8225	235	90619971
Haematotoxicity	86.07	21.67	35	8206	12500	90607706
Blast cell crisis	83.43	21.67	13	8228	73	90620133
Pericardial effusion	80.61	21.67	47	8194	36786	90583420
Graft versus host disease	74.50	21.67	28	8213	8116	90612090
Peripheral arterial occlusive disease	73.54	21.67	24	8217	4597	90615609
Leukaemia recurrent	70.44	21.67	18	8223	1449	90618757
Rash	68.55	21.67	192	8049	795908	89824298
Platelet count decreased	67.00	21.67	72	8169	136897	90483309
Lipase increased	66.07	21.67	28	8213	11083	90609123
Chronic myeloid leukaemia transformation	63.32	21.67	11	8230	130	90620076
Pleural effusion	60.34	21.67	62	8179	111929	90508277
Therapeutic response delayed	58.88	21.67	14	8227	836	90619370
Graft versus host disease in eye	57.89	21.67	10	8231	114	90620092
Pancytopenia	51.52	21.67	59	8182	120204	90500002
Stem cell transplant	50.29	21.67	15	8226	2139	90618067
Cytokine release syndrome	49.11	21.67	31	8210	27942	90592264
Philadelphia positive acute lymphocytic leukaemia	47.73	21.67	7	8234	24	90620182
Ischaemic stroke	45.12	21.67	27	8214	22139	90598067
Capillary leak syndrome	42.53	21.67	14	8227	2753	90617453
Bone pain	42.14	21.67	39	8202	61944	90558262
Product dose omission issue	41.90	21.67	86	8155	291601	90328605
Skin toxicity	40.02	21.67	17	8224	6762	90613444
Ichthyosis acquired	39.18	21.67	5	8236	3	90620203
Malignant neoplasm progression	38.47	21.67	48	8193	106822	90513384
Catabolic state	36.77	21.67	6	8235	47	90620159
Pancreatitis	36.40	21.67	38	8203	69788	90550418
Myalgia	35.63	21.67	60	8181	175065	90445141
Device related bacteraemia	34.82	21.67	8	8233	411	90619795
Minimal residual disease	34.54	21.67	8	8233	426	90619780
Ichthyosis	34.45	21.67	6	8235	72	90620134
Renal artery stenosis	33.40	21.67	11	8230	2166	90618040
Pyrexia	33.12	21.67	133	8108	660352	89959854
Product administered to patient of inappropriate age	31.96	21.67	13	8228	4640	90615566
Haemophagocytic lymphohistiocytosis	31.90	21.67	19	8222	15440	90604766
Febrile neutropenia	31.87	21.67	54	8187	158295	90461911
Cerebrovascular stenosis	31.01	21.67	5	8236	36	90620170
Off label use	30.95	21.67	188	8053	1102064	89518142
Skin exfoliation	30.22	21.67	34	8207	67879	90552327
Joint swelling	29.80	21.67	5	8236	503295	90116911
Hepatotoxicity	29.53	21.67	28	8213	45814	90574392
Hypertension	29.51	21.67	100	8141	457432	90162774
Graft versus host disease in skin	27.27	21.67	11	8230	3842	90616364
Chemotherapy	27.10	21.67	9	8232	1818	90618388
Peripheral artery stenosis	26.81	21.67	7	8234	613	90619593
Pityriasis rubra pilaris	25.69	21.67	5	8236	114	90620092
Swelling	25.16	21.67	4	8237	419054	90201152
Drug hypersensitivity	24.54	21.67	6	8235	463603	90156603
Granulicatella infection	24.34	21.67	5	8236	151	90620055
Chronic myeloid leukaemia	23.78	21.67	9	8232	2655	90617551
Hepatic function abnormal	23.78	21.67	25	8216	46263	90573943
Constipation	23.33	21.67	67	8174	280328	90339878
Blast cell count increased	23.01	21.67	6	8235	523	90619683
Platelet count abnormal	22.74	21.67	10	8231	4325	90615881
Sepsis	22.31	21.67	50	8191	179764	90440442
Splenomegaly	21.87	21.67	14	8227	12910	90607296

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
Acute lymphocytic leukaemia recurrent	397.14	20.70	105	10190	3586	42607454
Drug resistance	231.58	20.70	128	10167	34120	42576920
Philadelphia chromosome positive	221.89	20.70	47	10248	594	42610446
Blast crisis in myelogenous leukaemia	214.43	20.70	46	10249	620	42610420
Cytogenetic analysis abnormal	185.63	20.70	42	10253	733	42610307
Chronic myeloid leukaemia recurrent	167.59	20.70	32	10263	228	42610812
Neoplasm progression	147.13	20.70	90	10205	28910	42582130
Death	138.51	20.70	331	9964	470854	42140186
Drug intolerance	98.81	20.70	109	10186	80315	42530725
Blast cell crisis	84.79	20.70	16	10279	106	42610934
Autoimmune lymphoproliferative syndrome	81.36	20.70	17	10278	200	42610840
Lipase increased	67.24	20.70	38	10257	10528	42600512
Pancreatitis	64.40	20.70	65	10230	43203	42567837
Loss of therapeutic response	63.55	20.70	20	10275	1271	42609769
Central nervous system neoplasm	62.29	20.70	12	10283	90	42610950
Thrombocytopenia	61.21	20.70	139	10156	190140	42420900
Chronic myeloid leukaemia transformation	59.22	20.70	13	10282	196	42610844
Blast cells present	57.08	20.70	15	10280	498	42610542
Gallbladder oedema	56.80	20.70	13	10282	239	42610801
Viral haemorrhagic cystitis	56.45	20.70	20	10275	1834	42609206
Pleural effusion	56.01	20.70	91	10204	97075	42513965
Minimal residual disease	54.24	20.70	15	10280	606	42610434
Cytopenia	54.19	20.70	40	10255	17457	42593583
Peripheral arterial occlusive disease	47.34	20.70	26	10269	6812	42604228
Central nervous system leukaemia	46.18	20.70	12	10283	381	42610659
Hepatotoxicity	45.32	20.70	42	10253	25125	42585915
Acute lymphocytic leukaemia	44.52	20.70	20	10275	3411	42607629
Platelet count decreased	43.13	20.70	100	10195	138481	42472559
Stem cell transplant	42.57	20.70	18	10277	2654	42608386
Chronic myeloid leukaemia	40.41	20.70	17	10278	2475	42608565
Loss of CAR T-cell persistence	40.04	20.70	7	10288	28	42611012
Treatment failure	39.29	20.70	61	10234	62563	42548477
Leukaemic infiltration extramedullary	38.99	20.70	9	10286	172	42610868
Graft versus host disease	38.79	20.70	29	10266	12896	42598144
Periarthritis calcarea	38.78	20.70	8	10287	88	42610952
Articular calcification	38.45	20.70	8	10287	92	42610948
Cytokine release syndrome	36.13	20.70	49	10246	44478	42566562
Clonal evolution	36.06	20.70	8	10287	127	42610913
Renal artery stenosis	34.90	20.70	15	10280	2302	42608738
Myopathy toxic	34.49	20.70	11	10284	730	42610310
Hepatic calcification	33.20	20.70	9	10286	337	42610703
Adrenal cyst	33.09	20.70	8	10287	188	42610852
Bone marrow transplant	32.89	20.70	12	10283	1197	42609843
Haematopoietic stem cell mobilisation	32.80	20.70	9	10286	353	42610687
Bone pain	32.23	20.70	34	10261	23758	42587282
Gastrointestinal wall thickening	31.35	20.70	13	10282	1826	42609214
Costal cartilage fracture	31.28	20.70	8	10287	238	42610802
Adrenomegaly	31.18	20.70	9	10286	425	42610615
Renal artery angioplasty	31.15	20.70	5	10290	10	42611030
Post transplant lymphoproliferative disorder	30.85	20.70	22	10273	9098	42601942
Metamyelocyte count increased	30.51	20.70	9	10286	459	42610581
Immature granulocyte count increased	30.46	20.70	8	10287	265	42610775
Product dose omission issue	30.36	20.70	94	10201	154271	42456769
Renal artery stent placement	30.24	20.70	5	10290	13	42611027
Myeloid leukaemia	30.14	20.70	9	10286	479	42610561
Pericardial effusion	29.70	20.70	36	10259	29239	42581801
Epstein-Barr virus infection	29.60	20.70	22	10273	9696	42601344
Ichthyosis	29.57	20.70	7	10288	150	42610890
Hypertension	29.42	20.70	98	10197	167106	42443934
Dry skin	28.81	20.70	46	10249	48292	42562748
Red cell distribution width increased	28.76	20.70	19	10276	6945	42604095
Transplant	27.94	20.70	10	10285	944	42610096
Leukaemia recurrent	27.78	20.70	12	10283	1864	42609176
Pancytopenia	27.25	20.70	76	10219	117667	42493373
Myelocyte count increased	27.06	20.70	8	10287	411	42610629
Diarrhoea	26.70	20.70	44	10251	460805	42150235
Activated partial thromboplastin time shortened	25.80	20.70	8	10287	484	42610556
White blood cell count increased	25.63	20.70	42	10253	45045	42565995
Haematotoxicity	25.11	20.70	21	10274	10964	42600076
Adrenal adenoma	25.11	20.70	8	10287	529	42610511
Bone neoplasm	25.05	20.70	7	10288	294	42610746
Polymerase chain reaction positive	24.74	20.70	6	10289	143	42610897
Philadelphia positive acute lymphocytic leukaemia	24.23	20.70	5	10290	55	42610985
Malignant neoplasm progression	24.13	20.70	69	10226	108331	42502709
Leukaemic infiltration	23.71	20.70	6	10289	171	42610869
Graft versus host disease in gastrointestinal tract	23.62	20.70	15	10280	5128	42605912
Peripheral vascular disorder	23.16	20.70	15	10280	5302	42605738
Leukocytosis	23.05	20.70	32	10263	29676	42581364
Nephrocalcinosis	21.95	20.70	8	10287	795	42610245
Diaphragmatic disorder	21.94	20.70	9	10286	1230	42609810

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
Acute lymphocytic leukaemia recurrent	577.30	19.02	137	14253	5650	110569259
Drug resistance	295.68	19.02	145	14245	56229	110518680
Blast crisis in myelogenous leukaemia	289.48	19.02	57	14333	951	110573958
Philadelphia chromosome positive	283.58	19.02	55	14335	845	110574064
Death	210.93	19.02	347	14043	698522	109876387
Cytogenetic analysis abnormal	201.98	19.02	44	14346	1225	110573684
Chronic myeloid leukaemia recurrent	186.73	19.02	34	14356	363	110574546
Neoplasm progression	146.48	19.02	96	14294	64499	110510410
Thrombocytopenia	128.13	19.02	190	14200	348695	110226214
Lipase increased	122.24	19.02	56	14334	18616	110556293
Platelet count decreased	115.56	19.02	146	14244	230297	110344612
Central nervous system leukaemia	113.94	19.02	24	14366	567	110574342
Pleural effusion	107.73	19.02	124	14266	177585	110397324
Blast cell crisis	102.35	19.02	18	14372	155	110574754
Peripheral arterial occlusive disease	101.27	19.02	40	14350	9240	110565669
Cytopenia	99.62	19.02	57	14333	30059	110544850
Autoimmune lymphoproliferative syndrome	90.35	19.02	17	14373	220	110574689
Pericardial effusion	79.09	19.02	63	14327	57154	110517755
Graft versus host disease	77.07	19.02	41	14349	18765	110556144
Renal artery stenosis	74.08	19.02	25	14365	3701	110571208
Dry skin	73.55	19.02	80	14310	107573	110467336
Cytokine release syndrome	69.75	19.02	64	14326	70242	110504667
Stem cell transplant	66.11	19.02	24	14366	4403	110570506
Hepatotoxicity	65.41	19.02	59	14331	63341	110511568
Chronic myeloid leukaemia transformation	61.59	19.02	13	14377	310	110574599
Ichthyosis	60.83	19.02	12	14378	202	110574707
Pancytopenia	58.69	19.02	101	14289	209512	110365397
Minimal residual disease	57.06	19.02	15	14375	938	110573971
Haematotoxicity	56.90	19.02	35	14355	21047	110553862
Viral haemorrhagic cystitis	56.69	19.02	20	14370	3379	110571530
Leukaemia recurrent	54.43	19.02	19	14371	3112	110571797
Philadelphia positive acute lymphocytic leukaemia	52.22	19.02	9	14381	68	110574841
Pancreatitis	51.20	19.02	62	14328	93471	110481438
Febrile neutropenia	50.75	19.02	121	14269	316646	110258263
Loss of therapeutic response	50.52	19.02	17	14373	2493	110572416
Rash	47.68	19.02	222	14168	820742	109754167
Therapeutic response delayed	47.07	19.02	14	14376	1376	110573533
Graft versus host disease in eye	46.42	19.02	11	14379	449	110574460
Product administered to patient of inappropriate age	46.08	19.02	22	14368	8014	110566895
Bone marrow transplant	44.62	19.02	14	14376	1646	110573263
Neutrophil count decreased	44.45	19.02	66	14324	120875	110454034
Hypertension	43.97	19.02	156	14234	509928	110064981
Bone pain	43.76	19.02	48	14342	65085	110509824
Hepatic function abnormal	43.76	19.02	56	14334	89239	110485670
Neutropenia	43.57	19.02	127	14263	374493	110200416
Periarthritis calcarea	43.23	19.02	8	14382	94	110574815
Peripheral artery stenosis	43.10	19.02	13	14377	1341	110573568
Chronic myeloid leukaemia	41.71	19.02	17	14373	4256	110570653
Clonal evolution	41.57	19.02	9	14381	243	110574666
Pneumonia fungal	41.11	19.02	25	14365	14729	110560180
Adrenomegaly	40.60	19.02	10	14380	481	110574428
Joint swelling	40.50	19.02	5	14385	442840	110132069
Venoocclusive liver disease	40.41	19.02	25	14365	15182	110559727
Amylase increased	39.54	19.02	23	14367	12496	110562413
Drug hypersensitivity	39.46	19.02	6	14384	454084	110120825
Infusion related reaction	38.26	19.02	3	14387	381159	110193750
Hepatic calcification	38.25	19.02	9	14381	356	110574553
Gene mutation	38.18	19.02	15	14375	3414	110571495
Loss of CAR T-cell persistence	38.03	19.02	6	14384	24	110574885
Acute lymphocytic leukaemia	36.81	19.02	17	14373	5748	110569161
Haematopoietic stem cell mobilisation	36.72	19.02	9	14381	424	110574485
Articular calcification	35.98	19.02	8	14382	245	110574664
Costal cartilage fracture	35.73	19.02	8	14382	253	110574656
Adrenal cyst	35.67	19.02	8	14382	255	110574654
Pyrexia	35.13	19.02	218	14172	898047	109676862
Leukocytosis	35.01	19.02	39	14351	53789	110521120
Carotid artery stenosis	34.61	19.02	19	14371	9244	110565665
Swelling	34.57	19.02	3	14387	351038	110223871
Myeloid leukaemia	34.54	19.02	10	14380	895	110574014
Cerebral infarction	34.47	19.02	38	14352	51800	110523109
Ischaemic stroke	34.15	19.02	34	14356	41229	110533680
Blast cells present	33.77	19.02	10	14380	968	110573941
Leukaemic infiltration extramedullary	33.35	19.02	8	14382	344	110574565
Ichthyosis acquired	33.06	19.02	5	14385	14	110574895
Capillary leak syndrome	32.99	19.02	15	14375	4893	110570016
Coronary artery stenosis	32.51	19.02	21	14369	13737	110561172
Central nervous system neoplasm	32.48	19.02	7	14383	185	110574724
Metamyelocyte count increased	32.36	19.02	9	14381	697	110574212
Catabolic state	31.79	19.02	6	14384	79	110574830
Chronic graft versus host disease	31.53	19.02	18	14372	9439	110565470
Epstein-Barr virus infection	31.07	19.02	23	14367	18715	110556194
Renal artery angioplasty	30.62	19.02	5	14385	26	110574883
Post transplant lymphoproliferative disorder	30.09	19.02	21	14369	15592	110559317
Off label use	30	19.02	312	14078	1499873	109075036
Bone marrow leukaemic cell infiltration	29.93	19.02	6	14384	110	110574799
Pityriasis rubra pilaris	29.92	19.02	7	14383	270	110574639
Malignant neoplasm progression	29.35	19.02	68	14322	174499	110400410
Moyamoya disease	28.93	19.02	6	14384	131	110574778
Activated partial thromboplastin time shortened	28.77	19.02	9	14381	1048	110573861
Blast cell count increased	28.71	19.02	10	14380	1627	110573282
Skin toxicity	27.88	19.02	18	14372	11765	110563144
Full blood count decreased	27.59	19.02	27	14363	32072	110542837
Cerebrovascular stenosis	27.50	19.02	6	14384	168	110574741
Myopathy toxic	26.77	19.02	9	14381	1316	110573593
Immature granulocyte count increased	26.30	19.02	8	14382	849	110574060
Neoplasm recurrence	26.03	19.02	13	14377	5219	110569690
Carotid arteriosclerosis	25.92	19.02	11	14379	3046	110571863
Myelocyte count increased	25.79	19.02	8	14382	906	110574003
Splenomegaly	25.65	19.02	23	14367	24475	110550434
Red cell distribution width increased	25.64	19.02	20	14370	17582	110557327
Product dose omission issue	25.63	19.02	96	14294	321686	110253223
Peripheral vascular disorder	25.10	19.02	15	14375	8561	110566348
Renal artery stent placement	25.03	19.02	5	14385	90	110574819
Mesenteric arterial occlusion	24.79	19.02	6	14384	268	110574641
Blood bilirubin increased	24.44	19.02	39	14351	75933	110498976
Vascular occlusion	24.24	19.02	9	14381	1758	110573151
Skin exfoliation	24.19	19.02	42	14348	87609	110487300
White blood cell count decreased	24.02	19.02	75	14315	229315	110345594
Disease progression	23.93	19.02	78	14312	243956	110330953
Fall	23.88	19.02	26	14364	603456	109971453
Transaminases increased	23.86	19.02	35	14355	63355	110511554
Vomiting	23.82	19.02	52	14338	910623	109664286
Diaphragmatic disorder	23.67	19.02	9	14381	1877	110573032
Acquired gene mutation	23.65	19.02	10	14380	2744	110572165
Musculoskeletal stiffness	23.61	19.02	4	14386	279818	110295091
Abdominal discomfort	23.38	19.02	11	14379	393847	110181062
Graft versus host disease in skin	23.03	19.02	14	14376	8240	110566669
Confusional state	22.34	19.02	17	14373	468663	110106246
Bone marrow necrosis	22.09	19.02	6	14384	425	110574484
Granulicatella infection	22.07	19.02	5	14385	167	110574742
Adrenal adenoma	21.95	19.02	8	14382	1484	110573425
Condition aggravated	21.76	19.02	39	14351	734797	109840112
Constipation	21.59	19.02	98	14292	357688	110217221
Activated partial thromboplastin time prolonged	21.47	19.02	20	14370	22348	110552561
Angina pectoris	21.46	19.02	33	14357	62262	110512647
Acute coronary syndrome	20.91	19.02	20	14370	23092	110551817
Septic shock	20.82	19.02	56	14334	157472	110417437
Pancreatic enzymes increased	20.80	19.02	8	14382	1721	110573188
Wheezing	20.77	19.02	4	14386	255226	110319683
Maternal exposure during pregnancy	20.73	19.02	4	14386	254879	110320030
Nasopharyngitis	20.52	19.02	13	14377	394348	110180561
Bone marrow failure	20.43	19.02	31	14359	57817	110517092
Nephrocalcinosis	20.42	19.02	8	14382	1806	110573103
Urticaria	20.36	19.02	8	14382	318849	110256060
Abdominal pain	20.29	19.02	125	14265	512864	110062045
Haemangioma	20.18	19.02	9	14381	2807	110572102
Procalcitonin increased	19.95	19.02	10	14380	4046	110570863
Peripheral artery occlusion	19.91	19.02	9	14381	2896	110572013
Blister	19.75	19.02	3	14387	227373	110347536
Device related bacteraemia	19.61	19.02	7	14383	1223	110573686
Graft versus host disease in gastrointestinal tract	19.51	19.02	13	14377	8955	110565954
Transplant	19.37	19.02	7	14383	1267	110573642
Peripheral ischaemia	19.30	19.02	14	14376	11044	110563865
Acute myocardial infarction	19.14	19.02	37	14353	83740	110491169
Pancreatitis chronic	19.04	19.02	10	14380	4455	110570454

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EA05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS BCR-ABL tyrosine kinase inhibitors
FDA MoA	N0000175076	Protein Kinase Inhibitors
MeSH PA	D000092004	Tyrosine Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitor

Related Drugs by ATC class:

L01EA BCR-ABL tyrosine kinase inhibitors 5 drugs

asciminib bosutinib dasatinib imatinib nilotinib

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

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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.98	acidic
pKa2	8.49	Basic
pKa3	5.58	Basic
pKa4	4.36	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
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 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR THE TREATMENT OF LEUKEMIAS
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD OF TREATING CHRONIC MYELOGENOUS LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR THE TREATMENT OF LEUKEMIAS
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD OF TREATING CHRONIC MYELOGENOUS LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR THE TREATMENT OF LEUKEMIAS
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9029533	Dec. 22, 2026	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	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
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	11192897	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	11384086	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	11384086	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	11384086	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	9493470	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	9493470	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9493470	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9493470	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	9493470	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	9493470	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192895	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11192897	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING LEUKEMIA RESULTING FROM A MUTATION IN THE BCR-ABL KINASE DOMAIN
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	11384086	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9493470	Dec. 12, 2033	A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	9493470	Dec. 12, 2033	A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA

Orange Book exclusivity data (new drug applications)

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	March 19, 2027	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	March 19, 2027	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	March 19, 2027	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	March 19, 2027	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY
EQ 10MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 18, 2020	RX	TABLET	ORAL	March 19, 2031	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL)
EQ 15MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	March 19, 2031	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL)
EQ 30MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	April 23, 2015	RX	TABLET	ORAL	March 19, 2031	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL)
EQ 45MG BASE	ICLUSIG	TAKEDA PHARMS USA	N203469	Dec. 14, 2012	RX	TABLET	ORAL	March 19, 2031	TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL)

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN	INHIBITOR	IC50	9.43	WOMBAT-PK	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN	INHIBITOR	Kd	7.30	CHEMBL	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
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		IC50	9.52	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		IC50	7.59	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		IC50	8.43	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	8.82	WOMBAT-PK
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		IC50	8.07	CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN	INHIBITOR	IC50	8.96	WOMBAT-PK
Myosin light chain kinase, smooth muscle	Kinase	Q15746	MYLK_HUMAN		Kd	7	CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN		IC50	8.03	CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	7.09	CHEMBL
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN		IC50	7.49	CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN		IC50	7.94	CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		IC50	6.77	CHEMBL
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN	INHIBITOR	IC50	8.27	WOMBAT-PK
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN	INHIBITOR	IC50	9.62	WOMBAT-PK
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR	IC50	8.66	WOMBAT-PK
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	7.70	CHEMBL
Mitogen-activated protein kinase 11	Kinase	Q15759	MK11_HUMAN		Kd	6	CHEMBL
Ephrin type-A receptor 5	Kinase	P54756	EPHA5_HUMAN		Kd	8.10	CHEMBL
Ephrin type-A receptor 4	Kinase	P54764	EPHA4_HUMAN		Kd	4.77	CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		IC50	8.89	CHEMBL
TRAF2 and NCK-interacting protein kinase	Kinase	Q9UKE5	TNIK_HUMAN		Kd	6.42	CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	7.42	CHEMBL
Mitogen-activated protein kinase 14	Kinase	Q16539	MK14_HUMAN		Kd	6.81	CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	7.03	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	5.73	CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		IC50	8.17	CHEMBL
Cyclin-dependent kinase 8	Kinase	P49336	CDK8_HUMAN	INHIBITOR	Kd	8.17	IUPHAR
Cyclin-dependent kinase 16	Kinase	Q00536	CDK16_HUMAN		Kd	5.76	CHEMBL
Mitogen-activated protein kinase 9	Kinase	P45984	MK09_HUMAN		Kd	5.10	CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	5.75	CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	7.75	CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Kd	5.83	CHEMBL
TGF-beta receptor type-2	Kinase	P37173	TGFR2_HUMAN		Kd	5.75	CHEMBL
MAP kinase-activated protein kinase 2	Kinase	P49137	MAPK2_HUMAN		Kd	6.33	CHEMBL
Tyrosine-protein kinase BTK	Kinase	Q06187	BTK_HUMAN		Kd	5.74	CHEMBL
Ephrin type-B receptor 2	Kinase	P29323	EPHB2_HUMAN		Kd	5.73	CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	7.08	CHEMBL
Cyclin-dependent kinase 17	Kinase	Q00537	CDK17_HUMAN		Kd	6.47	CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	7.39	CHEMBL
Protein-tyrosine kinase 2-beta	Kinase	Q14289	FAK2_HUMAN		Kd	6.53	CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	5.53	CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	7.06	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	6.11	CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha	Kinase	P17612	KAPCA_HUMAN		IC50	6.21	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	6.51	CHEMBL
Cyclin-dependent kinase 19	Kinase	Q9BWU1	CDK19_HUMAN	INHIBITOR	Kd	7.92	IUPHAR
Ephrin type-A receptor 1	Kinase	P21709	EPHA1_HUMAN		Kd	5.94	CHEMBL
Ephrin type-B receptor 3	Kinase	P54753	EPHB3_HUMAN		Kd	6.26	CHEMBL
Receptor-interacting serine/threonine-protein kinase 1	Kinase	Q13546	RIPK1_HUMAN	INHIBITOR	IC50	7.92	IUPHAR
Fibroblast growth factor receptor 4	Kinase	P22455	FGFR4_HUMAN		IC50	8.15	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	7.39	CHEMBL
Interleukin-1 receptor-associated kinase 4	Kinase	Q9NWZ3	IRAK4_HUMAN		Kd	5.66	CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	6.16	CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	5.67	CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	5.76	CHEMBL
Mitogen-activated protein kinase kinase kinase 1	Kinase	Q13233	M3K1_HUMAN		Kd	6.31	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	5.53	CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2	Kinase	Q5S007	LRRK2_HUMAN		IC50	7.51	CHEMBL
Bcr/Abl fusion protein	Kinase	P00519 P11274	ABL1_HUMAN BCR_HUMAN		IC50	9.30	CHEMBL
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN	INHIBITOR	Ki	8.80	IUPHAR
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.11	CHEMBL
ATP-dependent RNA helicase DDX1	Enzyme	Q92499	DDX1_HUMAN		Kd	7.07	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	7.40	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase		SRC_CHICK		IC50	9.05	CHEMBL

External reference:

ID	Source
4340891KFS	UNII
D09950	KEGG_DRUG
4032031	VUID
N0000186141	NUI
4032031	VANDF
C2987417	UMLSCUI
CHEBI:78543	CHEBI
0LI	PDB_CHEM_ID
CHEMBL1171837	ChEMBL_ID
24826799	PUBCHEM_CID
DB08901	DRUGBANK_ID
CHEMBL2105708	ChEMBL_ID
9362	INN_ID
C545373	MESH_SUPPLEMENTAL_RECORD_UI
5890	IUPHAR_LIGAND_ID
1114544-31-8	SECONDARY_CAS_RN
1364347	RXNORM
196462	MMSL
29016	MMSL
31534	MMSL
d07936	MMSL
014797	NDDF
014798	NDDF
703796003	SNOMEDCT_US
703797007	SNOMEDCT_US
703798002	SNOMEDCT_US
4340891KFS	INXIGHT DRUGS

Pharmaceutical products:

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	63020-534	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	63020-536	TABLET, FILM COATED	10 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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ponatinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

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ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

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FDA Adverse Event Reporting System (Geriatric)

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🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

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