imatinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	1423	152459-95-5

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: imatinib gleevec imatinib mesylate imatinib mesilate CGP-57-148B CGP57148B CGP-57148 CGP57148 STI-571 STI571

A tyrosine kinase inhibitor and ANTINEOPLASTIC AGENT that inhibits the BCR-ABL kinase created by chromosome rearrangements in CHRONIC MYELOID LEUKEMIA and ACUTE LYMPHOBLASTIC LEUKEMIA, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors. Molecular weight: 493.62 Formula: C29H31N7O CLOGP: 4.38 LIPINSKI: 0 HAC: 8 HDO: 2 TPSA: 86.28 ALOGS: -4.53 ROTB: 7 Status: OFP 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	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	1 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	20.26 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	98 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	3.90 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	3.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	22 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Nov. 7, 2001	EMA	Novartis Europharm Limited
May 10, 2001	FDA	NOVARTIS

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
Death	1594.24	12.50	1622	38268	355610	52953566
Gastrointestinal stromal tumour	855.91	12.50	195	39695	1004	53308172
Chronic myeloid leukaemia	832.33	12.50	224	39666	2490	53306686
Blast crisis in myelogenous leukaemia	673.09	12.50	139	39751	403	53308773
Drug resistance	553.75	12.50	279	39611	19683	53289493
Cytogenetic analysis abnormal	543.91	12.50	124	39766	640	53308536
Malignant neoplasm progression	431.74	12.50	386	39504	71155	53238021
Second primary malignancy	424.20	12.50	170	39720	6962	53302214
Periorbital oedema	313.68	12.50	126	39764	5189	53303987
Gene mutation identification test positive	252.86	12.50	50	39840	107	53309069
Chronic myeloid leukaemia recurrent	227.53	12.50	49	39841	184	53308992
Neoplasm malignant	220.69	12.50	170	39720	25431	53283745
Philadelphia chromosome positive	219.66	12.50	51	39839	289	53308887
Rheumatoid arthritis	197.46	12.50	9	39881	314522	52994654
Muscle spasms	187.29	12.50	350	39540	134445	53174731
Chromosome analysis abnormal	183.75	12.50	38	39852	111	53309065
Pleural effusion	180.42	12.50	273	39617	88306	53220870
Leukaemia recurrent	174.85	12.50	58	39832	1369	53307807
Acute lymphocytic leukaemia recurrent	167.03	12.50	63	39827	2185	53306991
Chronic myeloid leukaemia transformation	166.37	12.50	35	39855	114	53309062
Oedema	162.67	12.50	237	39653	74109	53235067
Eyelid oedema	139.48	12.50	91	39799	10463	53298713
Gastric antral vascular ectasia	138.16	12.50	40	39850	590	53308586
Eye swelling	136.50	12.50	120	39770	21574	53287602
Bone marrow failure	113.62	12.50	126	39764	29989	53279187
Fluid retention	109.74	12.50	167	39723	54234	53254942
Nausea	108.20	12.50	946	38944	755145	52554031
Pancytopenia	103.11	12.50	217	39673	90711	53218465
Haematotoxicity	99.27	12.50	66	39824	7831	53301345
Face oedema	96.57	12.50	96	39794	20144	53289032
Conjunctival haemorrhage	94.76	12.50	47	39843	3197	53305979
Graft versus host disease	93.11	12.50	61	39829	7061	53302115
Drug hypersensitivity	93.01	12.50	41	39849	265201	53043975
Product substitution issue	92.35	12.50	84	39806	15782	53293394
Anaemia	91.35	12.50	429	39461	276289	53032887
Oedema peripheral	88.64	12.50	305	39585	170482	53138694
Arthropathy	85.64	12.50	5	39885	141448	53167728
Normal newborn	83.07	12.50	57	39833	7122	53302054
Gene mutation	81.20	12.50	32	39858	1251	53307925
Pseudoporphyria	80.50	12.50	20	39870	157	53309019
Completed suicide	80.38	12.50	6	39884	138195	53170981
Blast cell crisis	79.98	12.50	17	39873	59	53309117
Cytogenetic abnormality	78.06	12.50	25	39865	526	53308650
Generalised oedema	74.60	12.50	73	39817	15026	53294150
Thrombocytosis	73.83	12.50	48	39842	5484	53303692
Recurrent cancer	73.21	12.50	33	39857	1809	53307367
Metastases to liver	72.70	12.50	85	39805	21411	53287765
Growth retardation	70.54	12.50	28	39862	1116	53308060
Pain	69.50	12.50	218	39672	588180	52720996
Swelling face	68.96	12.50	140	39750	57028	53252148
Systemic lupus erythematosus	68.70	12.50	7	39883	125407	53183769
Acute lymphocytic leukaemia	67.74	12.50	36	39854	2829	53306347
Disease progression	67.45	12.50	198	39692	101722	53207454
Exposure via father	66.94	12.50	20	39870	331	53308845
Chronic graft versus host disease	66.43	12.50	37	39853	3191	53305985
Thrombocytopenia	65.29	12.50	240	39650	138487	53170689
Off label use	64.55	12.50	163	39727	472049	52837127
Rash	63.79	12.50	559	39331	445632	52863544
Pericardial effusion	62.58	12.50	89	39801	27189	53281987
Splenomegaly	62.18	12.50	56	39834	10383	53298793
Vomiting	62.10	12.50	605	39285	496534	52812642
Hepatotoxicity	61.08	12.50	89	39801	27791	53281385
Hypotension	58.76	12.50	62	39828	254014	53055162
Neoplasm recurrence	58.48	12.50	31	39859	2423	53306753
Therapeutic response decreased	57.97	12.50	117	39773	47452	53261724
Therapeutic product effect decreased	57.34	12.50	12	39878	125643	53183533
Bone pain	56.23	12.50	120	39770	50602	53258574
Neoplasm progression	54.95	12.50	88	39802	29831	53279345
Drug intolerance	54.65	12.50	300	39590	205193	53103983
Leukaemia	54.03	12.50	34	39856	3672	53305504
Diarrhoea	52.71	12.50	705	39185	624841	52684335
Polymerase chain reaction positive	51.98	12.50	12	39878	66	53309110
White blood cell count increased	51.95	12.50	110	39780	46135	53263041
Eye haemorrhage	49.07	12.50	43	39847	7691	53301485
Haemoglobin decreased	48.99	12.50	218	39672	137089	53172087
Confusional state	48.81	12.50	44	39846	194177	53114999
Fall	48.70	12.50	124	39766	358316	52950860
Therapy non-responder	48.56	12.50	111	39779	49009	53260167
Sinusitis	47.60	12.50	34	39856	168530	53140646
Exposure via body fluid	47.36	12.50	17	39873	511	53308665
Cardiac output decreased	46.58	12.50	20	39870	975	53308201
Lower respiratory tract infection	45.16	12.50	7	39883	90974	53218202
Glossodynia	44.90	12.50	10	39880	100281	53208895
Metastases to peritoneum	44.63	12.50	28	39862	3007	53306169
Platelet count increased	44.53	12.50	57	39833	15750	53293426
Eye oedema	44.43	12.50	22	39868	1491	53307685
Condition aggravated	44.16	12.50	98	39792	297036	53012140
Chordoma	43.40	12.50	7	39883	0	53309176
Neutropenia	43.37	12.50	234	39656	158951	53150225
Myalgia	43.22	12.50	206	39684	133285	53175891
Psoriasis	42.55	12.50	7	39883	87082	53222094
Joint swelling	41.27	12.50	70	39820	234568	53074608
Myelofibrosis	41.26	12.50	20	39870	1294	53307882
Urinary tract infection	40.00	12.50	74	39816	239829	53069347
Blast cells present	39.81	12.50	14	39876	396	53308780
Product use issue	39.60	12.50	28	39862	139556	53169620
Platelet count decreased	39.58	12.50	173	39717	107926	53201250
Exposure via partner	39.27	12.50	11	39879	143	53309033
Periorbital swelling	39.14	12.50	21	39869	1682	53307494
Overdose	38.75	12.50	16	39874	107720	53201456
Leukocytosis	37.77	12.50	67	39823	24667	53284509
Wound	37.39	12.50	11	39879	91546	53217630
Erythrocyanosis	37.20	12.50	6	39884	0	53309176
Asthma	36.35	12.50	18	39872	108954	53200222
Discomfort	36.29	12.50	13	39877	95459	53213717
Jaundice	36.26	12.50	74	39816	30239	53278937
Tumour excision	36.05	12.50	13	39877	396	53308780
Blast cell count increased	35.33	12.50	13	39877	420	53308756
Therapeutic response delayed	35.03	12.50	14	39876	568	53308608
Chloroma	34.96	12.50	11	39879	218	53308958
Peripheral arterial occlusive disease	33.49	12.50	26	39864	3928	53305248
Skin fragility	33.21	12.50	14	39876	652	53308524
Ascites	33.05	12.50	84	39806	39651	53269525
Bone marrow oedema	32.58	12.50	15	39875	864	53308312
Bone marrow transplant	32.06	12.50	14	39876	711	53308465
Acute graft versus host disease	31.48	12.50	26	39864	4291	53304885
Gastrointestinal toxicity	31.27	12.50	27	39863	4735	53304441
White blood cell count decreased	31.23	12.50	179	39711	124296	53184880
Pneumatosis intestinalis	31.23	12.50	20	39870	2226	53306950
Pulse waveform abnormal	31.23	12.50	8	39882	72	53309104
Loss of personal independence in daily activities	31.16	12.50	7	39883	69808	53239368
Ankle brachial index decreased	31.13	12.50	8	39882	73	53309103
Trisomy 8	31.00	12.50	5	39885	0	53309176
Blood lactate dehydrogenase increased	30.71	12.50	57	39833	21724	53287452
Carotid intima-media thickness increased	30.65	12.50	8	39882	78	53309098
Cardiotoxicity	30.07	12.50	32	39858	7267	53301909
Nasopharyngitis	29.71	12.50	62	39828	192233	53116943
Breast cancer	28.98	12.50	92	39798	49266	53259910
Toxic skin eruption	28.86	12.50	42	39848	13097	53296079
Right ventricular failure	28.83	12.50	48	39842	16795	53292381
Musculoskeletal stiffness	28.60	12.50	30	39860	123338	53185838
Typhoid fever	28.19	12.50	6	39884	21	53309155
Surgery	28.08	12.50	69	39821	31895	53277281
Intentional overdose	27.57	12.50	8	39882	67197	53241979
Acute kidney injury	27.14	12.50	98	39792	253770	53055406
Morphoea	26.83	12.50	10	39880	335	53308841
Left ventricular dysfunction	26.26	12.50	37	39853	11200	53297976
Aplasia	25.98	12.50	23	39867	4169	53305007
Chronic graft versus host disease in skin	25.92	12.50	12	39878	700	53308476
Anxiety	25.18	12.50	70	39820	196634	53112542
Dizziness	25.17	12.50	169	39721	372090	52937086
Tumour haemorrhage	24.90	12.50	15	39875	1499	53307677
Pubertal failure	24.89	12.50	5	39885	12	53309164
Slit-lamp tests abnormal	24.80	12.50	4	39886	0	53309176
Peritoneal lesion	24.80	12.50	4	39886	0	53309176
Hypersensitivity	24.78	12.50	78	39812	210587	53098589
Tumour necrosis	24.64	12.50	12	39878	784	53308392
Transdifferentiation of neoplasm	24.60	12.50	5	39885	13	53309163
Blood pressure increased	24.59	12.50	42	39848	140437	53168739
Cytopenia	24.16	12.50	32	39858	9138	53300038
Urine odour abnormal	24.07	12.50	25	39865	5521	53303655
Syncope	24.03	12.50	29	39861	111964	53197212
Pyrexia	24.02	12.50	429	39461	402764	52906412
Back pain	24.00	12.50	92	39798	234155	53075021
Hepatic necrosis	23.32	12.50	25	39865	5725	53303451
Abortion	23.24	12.50	17	39873	2349	53306827
Abortion spontaneous	23.02	12.50	82	39808	46553	53262623
Injury	22.97	12.50	5	39885	50966	53258210
Hallucination	22.85	12.50	6	39884	53832	53255344
Leukopenia	22.77	12.50	112	39778	73351	53235825
Somnolence	22.75	12.50	58	39832	167676	53141500
Intentional product use issue	22.67	12.50	13	39877	72481	53236695
Inappropriate schedule of product administration	22.61	12.50	14	39876	74864	53234312
Agitation	22.24	12.50	8	39882	58618	53250558
Papilloedema	22.13	12.50	20	39870	3723	53305453
Liver disorder	21.90	12.50	73	39817	40082	53269094
Therapy partial responder	21.89	12.50	25	39865	6138	53303038
Suicidal ideation	21.73	12.50	9	39881	60502	53248674
Arthritis	21.64	12.50	20	39870	87278	53221898
Insomnia	21.48	12.50	70	39820	187002	53122174
Hyponatraemia	21.37	12.50	30	39860	108577	53200599
Basophilia	21.14	12.50	4	39886	6	53309170
Pericarditis	20.93	12.50	11	39879	64395	53244781
Tremor	20.74	12.50	39	39851	125697	53183479
Chylothorax	20.51	12.50	8	39882	304	53308872
Intracardiac mass	20.50	12.50	5	39885	36	53309140
Anaphylactic reaction	20.42	12.50	9	39881	58317	53250859
Oral pigmentation	20.41	12.50	4	39886	8	53309168
Therapy interrupted	20.41	12.50	45	39845	19391	53289785
Hypertension	20.33	12.50	93	39797	225338	53083838
Gastric cancer	20.25	12.50	18	39872	3279	53305897
Flushing	20.23	12.50	14	39876	70586	53238590
Drug ineffective	20.16	12.50	462	39428	816783	52492393
Microangiopathy	19.92	12.50	11	39879	933	53308243
Blood test abnormal	19.83	12.50	33	39857	11544	53297632
Stem cell transplant	19.82	12.50	14	39876	1831	53307345
Computerised tomogram abnormal	19.65	12.50	15	39875	2211	53306965
Exposure during pregnancy	19.61	12.50	160	39730	124700	53184476
Neoplasm	19.50	12.50	24	39866	6372	53302804
Lacrimation increased	19.42	12.50	42	39848	17861	53291315
Urticaria	19.19	12.50	46	39844	135839	53173337
Obliterative bronchiolitis	19.13	12.50	14	39876	1936	53307240
Exophthalmos	18.83	12.50	12	39878	1324	53307852
Acute myeloid leukaemia	18.69	12.50	40	39850	16892	53292284
Aspiration pleural cavity	18.56	12.50	10	39880	808	53308368
Fibromyalgia	18.54	12.50	5	39885	44070	53265106
Product dose omission issue	18.52	12.50	77	39813	191543	53117633
Jaw operation	18.50	12.50	10	39880	813	53308363
Myelocytosis	18.37	12.50	4	39886	16	53309160
Mobility decreased	18.29	12.50	18	39872	76253	53232923
Cellulitis	18.15	12.50	18	39872	75971	53233205
Gastrointestinal angiectasia	17.85	12.50	5	39885	65	53309111
Disseminated intravascular coagulation	17.78	12.50	43	39847	19676	53289500
Eosinophilia	17.63	12.50	45	39845	21290	53287886
Dengue fever	17.59	12.50	9	39881	654	53308522
Influenza like illness	17.52	12.50	12	39878	60847	53248329
Loss of consciousness	17.48	12.50	37	39853	114175	53195001
Scleroderma-like reaction	17.19	12.50	5	39885	75	53309101
Therapy cessation	17.15	12.50	53	39837	27972	53281204
Pigmentation disorder	17.05	12.50	18	39872	4049	53305127
Headache	16.96	12.50	291	39599	536530	52772646
Hyperhidrosis	16.88	12.50	29	39861	96764	53212412
Hepatic failure	16.85	12.50	62	39828	35744	53273432
Hyperkalaemia	16.58	12.50	10	39880	54246	53254930
Ejection fraction decreased	16.54	12.50	42	39848	19806	53289370
Metastasis	16.48	12.50	19	39871	4712	53304464
Fibrin degradation products increased	16.45	12.50	6	39884	189	53308987
Acquired gene mutation	16.24	12.50	9	39881	768	53308408
Deep vein thrombosis	16.21	12.50	23	39867	82890	53226286
Lichen planus	16.19	12.50	13	39877	2061	53307115
Abortion induced	16.11	12.50	29	39861	10797	53298379
Swelling of eyelid	15.96	12.50	12	39878	1728	53307448
Dry skin	15.80	12.50	72	39818	45688	53263488
Blood blister	15.78	12.50	12	39878	1759	53307417
Knee arthroplasty	15.73	12.50	3	39887	33566	53275610
Tumour lysis syndrome	15.62	12.50	24	39866	7850	53301326
Aspartate aminotransferase increased	15.60	12.50	112	39778	83917	53225259
Philadelphia positive chronic myeloid leukaemia	15.52	12.50	4	39886	37	53309139
Central nervous system leukaemia	15.49	12.50	5	39885	108	53309068
Helicobacter infection	15.39	12.50	5	39885	39064	53270112
Lichenoid keratosis	15.21	12.50	11	39879	1494	53307682
Acute leukaemia	15.19	12.50	10	39880	1166	53308010
Pulmonary embolism	15.18	12.50	40	39850	114402	53194774
Acute myeloid leukaemia recurrent	15.15	12.50	11	39879	1502	53307674
Delirium	15.14	12.50	6	39884	41423	53267753
Hepatic mass	15.10	12.50	11	39879	1510	53307666
Ocular hyperaemia	15.03	12.50	43	39847	21748	53287428
Subdural haematoma evacuation	14.99	12.50	3	39887	7	53309169
Food interaction	14.86	12.50	8	39882	645	53308531
Type 2 diabetes mellitus	14.49	12.50	3	39887	31667	53277509
Impaired healing	14.44	12.50	16	39874	64189	53244987
Osteoarthritis	14.33	12.50	19	39871	70467	53238709
Irritability	14.02	12.50	3	39887	30950	53278226
Cystitis	13.89	12.50	9	39881	46979	53262197
Myeloid maturation arrest	13.78	12.50	3	39887	12	53309164
Dermatofibrosarcoma protuberans	13.78	12.50	3	39887	12	53309164
Blood bilirubin increased	13.69	12.50	58	39832	35672	53273504
Suicide attempt	13.63	12.50	14	39876	58154	53251022
Oncologic complication	13.58	12.50	5	39885	162	53309014
Primary adrenal insufficiency	13.57	12.50	4	39886	63	53309113
Cardiac failure	13.47	12.50	110	39780	85734	53223442
Adenocarcinoma gastric	13.46	12.50	7	39883	526	53308650
Growth failure	13.39	12.50	6	39884	324	53308852
Polyhydramnios	13.38	12.50	12	39878	2213	53306963
Bone metabolism disorder	13.34	12.50	6	39884	327	53308849
Gastrectomy	13.28	12.50	7	39883	541	53308635
Hepatic enzyme increased	13.28	12.50	49	39841	126146	53183030
Desmoid tumour	13.18	12.50	4	39886	70	53309106
Hepatomegaly	13.11	12.50	28	39862	11803	53297373
Leukaemic infiltration extramedullary	13.07	12.50	4	39886	72	53309104
Therapeutic product effect incomplete	13.01	12.50	31	39859	91753	53217423
Therapy responder	13.01	12.50	6	39884	347	53308829
Hepatic neoplasm	12.92	12.50	11	39879	1893	53307283
Drug level increased	12.85	12.50	39	39851	20382	53288794
Complications of transplant surgery	12.85	12.50	5	39885	189	53308987
Skin hypopigmentation	12.83	12.50	7	39883	580	53308596
Skull fractured base	12.82	12.50	4	39886	77	53309099
Red blood cell count decreased	12.78	12.50	57	39833	35846	53273330
Central nervous system neoplasm	12.77	12.50	3	39887	18	53309158
Blood alkaline phosphatase increased	12.77	12.50	63	39827	41299	53267877
Arthralgia	12.73	12.50	242	39648	439541	52869635
Balance disorder	12.70	12.50	22	39868	73185	53235991
Blood creatine phosphokinase increased	12.66	12.50	49	39841	28936	53280240
Myelodysplastic syndrome	12.60	12.50	34	39856	16626	53292550
Therapy change	12.56	12.50	18	39872	5534	53303642
Vaccination failure	12.53	12.50	5	39885	202	53308974
Seizure	12.53	12.50	52	39838	129457	53179719

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
Death	2388.69	12.34	2694	40045	379823	32090964
Gastrointestinal stromal tumour	1153.30	12.34	281	42458	1029	32469758
Chronic myeloid leukaemia	1066.48	12.34	309	42430	2475	32468312
Drug resistance	825.31	12.34	460	42279	22505	32448282
Blast crisis in myelogenous leukaemia	729.57	12.34	167	42572	429	32470358
Second primary malignancy	607.41	12.34	256	42483	6685	32464102
Malignant neoplasm progression	491.14	12.34	559	42180	77937	32392850
Cytogenetic analysis abnormal	442.18	12.34	109	42630	423	32470364
Neoplasm malignant	376.18	12.34	260	42479	18625	32452162
Philadelphia chromosome positive	297.86	12.34	72	42667	252	32470535
Pleural effusion	224.28	12.34	385	42354	78607	32392180
Drug intolerance	211.71	12.34	294	42445	49941	32420846
Gene mutation	198.68	12.34	67	42672	919	32469868
Chromosome analysis abnormal	197.97	12.34	43	42696	78	32470709
Acute lymphocytic leukaemia recurrent	193.49	12.34	90	42649	2982	32467805
Periorbital oedema	157.82	12.34	82	42657	3466	32467321
Leukaemia recurrent	155.25	12.34	64	42675	1575	32469212
Chronic myeloid leukaemia transformation	154.22	12.34	38	42701	147	32470640
Metastases to liver	151.62	12.34	130	42609	12802	32457985
Chronic myeloid leukaemia recurrent	149.58	12.34	37	42702	146	32470641
Gene mutation identification test positive	130.76	12.34	34	42705	171	32470616
Therapeutic response decreased	114.06	12.34	155	42584	25765	32445022
Recurrent cancer	105.83	12.34	45	42694	1199	32469588
Oedema	105.01	12.34	202	42537	44945	32425842
Chronic graft versus host disease	102.40	12.34	67	42672	4373	32466414
White blood cell count increased	98.45	12.34	187	42552	41215	32429572
Blast cell crisis	98.08	12.34	23	42716	68	32470719
Eyelid oedema	96.35	12.34	69	42670	5220	32465567
Hypotension	93.40	12.34	88	42651	216022	32254765
Muscle spasms	91.24	12.34	250	42489	70168	32400619
Drug abuse	88.51	12.34	4	42735	80239	32390548
Acute lymphocytic leukaemia	88.32	12.34	56	42683	3462	32467325
Neoplasm recurrence	87.30	12.34	46	42693	2001	32468786
Completed suicide	81.96	12.34	12	42727	92505	32378282
Neoplasm progression	81.14	12.34	114	42625	19544	32451243
Blast cells present	79.21	12.34	29	42710	513	32470274
Acute kidney injury	77.84	12.34	169	42570	293299	32177488
Overdose	77.82	12.34	11	42728	87066	32383721
Polymerase chain reaction positive	76.69	12.34	20	42719	102	32470685
Gastric antral vascular ectasia	76.42	12.34	25	42714	310	32470477
Therapy non-responder	74.56	12.34	145	42594	32509	32438278
Desmoid tumour	74.18	12.34	19	42720	89	32470698
Splenomegaly	68.93	12.34	90	42649	14387	32456400
Chordoma	67.63	12.34	12	42727	0	32470787
Necrotising panniculitis	67.45	12.34	15	42724	32	32470755
Face oedema	66.93	12.34	80	42659	11695	32459092
Graft versus host disease	62.38	12.34	74	42665	10732	32460055
Clonal evolution	61.12	12.34	17	42722	115	32470672
Scleroderma	60.81	12.34	32	42707	1388	32469399
Fluid retention	59.51	12.34	117	42622	26433	32444354
Acquired gene mutation	58.86	12.34	30	42709	1217	32469570
Fall	58.82	12.34	105	42634	196096	32274691
Product substitution issue	57.84	12.34	70	42669	10366	32460421
Blast cell count increased	56.55	12.34	28	42711	1067	32469720
Metastases to peritoneum	56.02	12.34	32	42707	1634	32469153
Prostate cancer	55.75	12.34	116	42623	27290	32443497
Bradycardia	55.42	12.34	13	42726	71549	32399238
Central nervous system leukaemia	51.17	12.34	18	42721	282	32470505
Confusional state	51.10	12.34	68	42671	143047	32327740
Off label use	50.68	12.34	219	42520	306101	32164686
Cytogenetic abnormality	50.15	12.34	24	42715	848	32469939
Disease progression	48.98	12.34	235	42504	86627	32384160
Myelofibrosis	47.94	12.34	29	42710	1648	32469139
Bone pain	47.23	12.34	91	42648	20253	32450534
Treatment failure	46.71	12.34	135	42604	39028	32431759
Accident	45.40	12.34	40	42699	4082	32466705
Bone marrow necrosis	45.07	12.34	14	42725	145	32470642
Hyperkalaemia	44.45	12.34	18	42721	69732	32401055
Central nervous system neoplasm	44.09	12.34	12	42727	74	32470713
Endocarditis noninfective	43.99	12.34	13	42726	112	32470675
Pituitary apoplexy	43.31	12.34	10	42729	27	32470760
Exposure via father	42.72	12.34	13	42726	125	32470662
Haemoglobin decreased	42.47	12.34	286	42453	119385	32351402
Bone marrow failure	42.41	12.34	111	42628	30293	32440494
Typhoid fever	42.29	12.34	10	42729	31	32470756
Chronic graft versus host disease in skin	42.11	12.34	21	42718	813	32469974
Thrombocytopenia	41.55	12.34	335	42404	147964	32322823
Somnolence	40.52	12.34	46	42693	103751	32367036
Intentional overdose	40.25	12.34	4	42735	41597	32429190
Pulmonary embolism	39.79	12.34	31	42708	83628	32387159
Tumour haemorrhage	39.23	12.34	31	42708	2720	32468067
Surgery	39.10	12.34	64	42675	12535	32458252
Platelet count decreased	38.37	12.34	270	42469	114321	32356466
Ascites	38.17	12.34	128	42611	40063	32430724
Hallucination	37.98	12.34	11	42728	52608	32418179
Tumour rupture	36.65	12.34	13	42726	209	32470578
Toxicity to various agents	36.08	12.34	117	42622	177924	32292863
Loss of therapeutic response	35.09	12.34	13	42726	238	32470549
Tumour necrosis	34.53	12.34	21	42718	1205	32469582
Colon cancer	34.49	12.34	50	42689	8816	32461971
Generalised oedema	34.22	12.34	60	42679	12423	32458364
Syncope	34.03	12.34	41	42698	90083	32380704
Nausea	33.28	12.34	599	42140	320250	32150537
Gastrectomy	32.81	12.34	11	42728	148	32470639
Drug hypersensitivity	32.68	12.34	29	42710	73371	32397416
Gastric cancer	32.65	12.34	38	42701	5399	32465388
Seizure	32.51	12.34	54	42685	103800	32366987
Pneumonia	32.37	12.34	305	42434	354947	32115840
Delirium	32.17	12.34	9	42730	44037	32426750
Cardiac arrest	31.54	12.34	49	42690	96727	32374060
Pulmonary aplasia	31.39	12.34	6	42733	3	32470784
Tuberculosis	30.76	12.34	47	42692	8682	32462105
Rhabdomyolysis	30.64	12.34	26	42713	67239	32403548
Inappropriate schedule of product administration	30.56	12.34	11	42728	45814	32424973
Dizziness	30.40	12.34	157	42582	209461	32261326
Eye swelling	30.22	12.34	49	42690	9523	32461264
Growth retardation	30.11	12.34	22	42717	1717	32469070
Pericardial effusion	30.08	12.34	82	42657	22920	32447867
Pemphigus	30.06	12.34	20	42719	1342	32469445
Deep vein thrombosis	29.80	12.34	24	42715	63689	32407098
Tumour excision	29.79	12.34	10	42729	135	32470652
Oral pigmentation	29.66	12.34	6	42733	6	32470781
Psoriasis	29.22	12.34	12	42727	46111	32424676
Chloroma	29.14	12.34	14	42725	499	32470288
Anxiety	29.06	12.34	51	42688	95954	32374833
Tremor	28.59	12.34	39	42700	81238	32389549
Demyelination	28.57	12.34	26	42713	2768	32468019
Loss of CAR T-cell persistence	28.22	12.34	7	42732	28	32470759
Renal tuberculosis	28.18	12.34	5	42734	0	32470787
Graft versus host disease in eye	27.82	12.34	11	42728	242	32470545
Flushing	27.63	12.34	4	42735	31123	32439664
Stem cell transplant	27.34	12.34	23	42716	2204	32468583
Oedema peripheral	27.33	12.34	249	42490	113842	32356945
Drug interaction	27.02	12.34	172	42567	218013	32252774
Pseudoporphyria	27.01	12.34	11	42728	262	32470525
Metabolic acidosis	26.75	12.34	10	42729	40689	32430098
Drug clearance decreased	26.42	12.34	19	42720	1446	32469341
Malaria	26.41	12.34	11	42728	278	32470509
Hyperhidrosis	26.21	12.34	33	42706	71135	32399652
Blindness	26.03	12.34	55	42684	13071	32457716
Optic neuritis	26.02	12.34	27	42712	3375	32467412
Blood lactate dehydrogenase increased	25.83	12.34	75	42664	21730	32449057
Plasma cell myeloma	25.36	12.34	23	42716	57591	32413196
Therapeutic product effect decreased	25.29	12.34	5	42734	31012	32439775
Metamyelocyte count increased	25.15	12.34	12	42727	421	32470366
Blood pressure increased	25.07	12.34	41	42698	79313	32391474
International normalised ratio increased	24.83	12.34	17	42722	49018	32421769
Haematotoxicity	24.61	12.34	37	42702	6739	32464048
Chronic obstructive pulmonary disease	24.55	12.34	17	42722	48736	32422051
Bone marrow disorder	24.33	12.34	19	42720	1639	32469148
Rash	23.87	12.34	397	42342	208936	32261851
Agitation	23.85	12.34	24	42715	57212	32413575
Post embolisation syndrome	23.22	12.34	7	42732	65	32470722
Bone marrow transplant	22.80	12.34	15	42724	988	32469799
Bone neoplasm	22.76	12.34	10	42729	289	32470498
Right ventricular diastolic collapse	22.76	12.34	7	42732	70	32470717
Cardio-respiratory arrest	22.73	12.34	24	42715	55965	32414822
Epistaxis	22.61	12.34	24	42715	55831	32414956
Dehydration	22.61	12.34	90	42649	128868	32341919
Spleen palpable	22.54	12.34	4	42735	0	32470787
Acute aortic syndrome	22.54	12.34	4	42735	0	32470787
Philadelphia chromosome negative	22.54	12.34	4	42735	0	32470787
Anaphylactic reaction	22.34	12.34	6	42733	30166	32440621
Aggression	22.25	12.34	12	42727	39377	32431410
Large intestine infection	22.21	12.34	17	42722	1423	32469364
Graft versus host disease in lung	22.03	12.34	12	42727	558	32470229
Urticaria	21.58	12.34	28	42711	59586	32411201
B-cell small lymphocytic lymphoma	21.57	12.34	8	42731	147	32470640
Pancytopenia	21.27	12.34	198	42541	91037	32379750
Arterial disorder	21.26	12.34	16	42723	1306	32469481
Philadelphia positive chronic myeloid leukaemia	21.24	12.34	7	42732	89	32470698
Ocular myasthenia	21.19	12.34	9	42730	239	32470548
Dengue fever	21.02	12.34	9	42730	244	32470543
Therapy partial responder	20.94	12.34	29	42710	4901	32465886
Suicidal ideation	20.94	12.34	12	42727	38071	32432716
Drug dependence	20.89	12.34	3	42736	23481	32447306
Condition aggravated	20.66	12.34	120	42619	155541	32315246
Rectosigmoid cancer	20.40	12.34	8	42731	172	32470615
Neoplasm	20.39	12.34	27	42712	4374	32466413
Complications of transplant surgery	20.33	12.34	11	42728	505	32470282
Myelocyte count increased	19.93	12.34	10	42729	392	32470395
Suicide attempt	19.71	12.34	13	42726	38231	32432556
Transformation to acute myeloid leukaemia	19.65	12.34	12	42727	694	32470093
Bone marrow oedema	19.45	12.34	11	42728	551	32470236
Peripheral arterial occlusive disease	19.08	12.34	30	42709	5679	32465108
Intentional product misuse	18.92	12.34	12	42727	36039	32434748
Tachycardia	18.90	12.34	48	42691	79040	32391747
Pericardial excision	18.89	12.34	4	42735	6	32470781
Multiple-drug resistance	18.80	12.34	24	42715	3751	32467036
Diaphragmatic disorder	18.75	12.34	14	42725	1129	32469658
Cytopenia	18.62	12.34	41	42698	10023	32460764
Mental status changes	18.48	12.34	14	42725	38323	32432464
Wheezing	18.38	12.34	13	42726	36861	32433926
Chest expansion decreased	18.32	12.34	7	42732	140	32470647
Acoustic neuroma	18.23	12.34	7	42732	142	32470645
Hyponatraemia	17.98	12.34	45	42694	74468	32396319
Concomitant disease aggravated	17.92	12.34	29	42710	5624	32465163
Lactic acidosis	17.83	12.34	11	42728	33525	32437262
Leukaemia	17.77	12.34	24	42715	3962	32466825
Asthma	17.76	12.34	19	42720	44046	32426741
Medication error	17.62	12.34	4	42735	22531	32448256
Platelet count increased	17.61	12.34	38	42701	9163	32461624
Neuropathy peripheral	17.43	12.34	48	42691	76934	32393853
Hepatic calcification	17.41	12.34	9	42730	376	32470411
Acinetobacter sepsis	17.36	12.34	5	42734	39	32470748
Marrow hyperplasia	17.30	12.34	13	42726	1059	32469728
Therapy change	17.28	12.34	20	42719	2825	32467962
Gelatinous transformation of the bone marrow	17.27	12.34	4	42735	11	32470776
Vomiting	17.21	12.34	418	42321	235139	32235648
Encephalopathy	17.17	12.34	12	42727	34245	32436542
Atrial fibrillation	17.11	12.34	87	42652	116617	32354170
Stress	17.11	12.34	5	42734	23777	32447010
Myeloproliferative neoplasm	17.04	12.34	10	42729	537	32470250
Adrenomegaly	16.94	12.34	9	42730	398	32470389
Pseudomyxoma peritonei	16.91	12.34	3	42736	0	32470787
Janus kinase 2 mutation	16.91	12.34	3	42736	0	32470787
Hepatic embolisation	16.91	12.34	3	42736	0	32470787
Cytoreductive surgery	16.91	12.34	3	42736	0	32470787
Hydrocele operation	16.91	12.34	3	42736	0	32470787
Drug reaction with eosinophilia and systemic symptoms	16.79	12.34	11	42728	32474	32438313
Abscess drainage	16.79	12.34	8	42731	280	32470507
Paternal exposure during pregnancy	16.77	12.34	4	42735	13	32470774
Anaemia	16.69	12.34	398	42341	223226	32247561
Costal cartilage fracture	16.53	12.34	8	42731	290	32470497
Blood pressure decreased	16.50	12.34	26	42713	51054	32419733
Coma	16.49	12.34	19	42720	42593	32428194
Product dose omission issue	16.48	12.34	74	42665	102501	32368286
Constipation	16.46	12.34	98	42641	126275	32344512
Periorbital swelling	16.35	12.34	8	42731	297	32470490
Essential thrombocythaemia	16.26	12.34	5	42734	50	32470737
Biopsy bone marrow abnormal	16.23	12.34	8	42731	302	32470485
Lung neoplasm malignant	16.19	12.34	52	42687	15911	32454876
Intentional product use issue	16.14	12.34	19	42720	42192	32428595
Pigmentation disorder	15.93	12.34	17	42722	2195	32468592
Cellulitis	15.82	12.34	26	42713	50204	32420583
Insomnia	15.76	12.34	73	42666	100275	32370512
Growth failure	15.67	12.34	5	42734	57	32470730
Colitis	15.61	12.34	13	42726	33938	32436849
Trisomy 8	15.36	12.34	5	42734	61	32470726
Lactose intolerance	15.11	12.34	13	42726	1285	32469502
Thrombosis	15.05	12.34	23	42716	45731	32425056
Intestinal congestion	14.94	12.34	4	42735	23	32470764
Bladder cancer	14.87	12.34	38	42701	10218	32460569
Metastases to bladder	14.86	12.34	5	42734	68	32470719
Bence Jones proteinuria	14.83	12.34	3	42736	3	32470784
Metastases to heart	14.58	12.34	6	42733	147	32470640
Hypereosinophilic syndrome	14.53	12.34	7	42732	251	32470536
Parakeratosis	14.46	12.34	6	42733	150	32470637
Product prescribing error	14.45	12.34	4	42735	19713	32451074
Angioedema	14.24	12.34	16	42723	36273	32434514
Disease recurrence	14.23	12.34	50	42689	16014	32454773
Lacrimation increased	14.14	12.34	31	42708	7553	32463234
Hyperchromic anaemia	14.14	12.34	4	42735	29	32470758
Product use in unapproved indication	14.14	12.34	176	42563	87028	32383759
Unevaluable event	14.08	12.34	14	42725	33572	32437215
Loss of personal independence in daily activities	13.99	12.34	9	42730	26824	32443963
Aspiration bone marrow	13.62	12.34	3	42736	6	32470781
Clear cell sarcoma of soft tissue	13.62	12.34	3	42736	6	32470781
Gastric neoplasm	13.47	12.34	5	42734	92	32470695
Leukostasis syndrome	13.38	12.34	4	42735	36	32470751
Therapy responder	13.32	12.34	6	42733	184	32470603
Metastasis	13.32	12.34	20	42719	3637	32467150
Pneumonia aspiration	13.24	12.34	21	42718	41135	32429652
Oropharyngeal pain	13.22	12.34	13	42726	31339	32439448
Ejection fraction decreased	13.16	12.34	52	42687	17606	32453181
Bladder neoplasm surgery	13.09	12.34	4	42735	39	32470748
Blast cell proliferation	13.02	12.34	3	42736	8	32470779
Transitional cell carcinoma	13.00	12.34	15	42724	2112	32468675
Hypoglycaemia	12.99	12.34	33	42706	54349	32416438
Cancer surgery	12.88	12.34	8	42731	477	32470310
Hypertension	12.85	12.34	111	42628	131639	32339148
Orthostatic hypotension	12.84	12.34	9	42730	25641	32445146
Bone development abnormal	12.83	12.34	4	42735	42	32470745
Ventricular tachycardia	12.75	12.34	9	42730	25547	32445240
Chills	12.74	12.34	56	42683	78028	32392759
Musculoskeletal stiffness	12.66	12.34	20	42719	39244	32431543
Drug-induced liver injury	12.64	12.34	8	42731	24055	32446732
Laryngeal cancer stage III	12.52	12.34	3	42736	10	32470777
Breast oedema	12.52	12.34	3	42736	10	32470777
Hyperkeratosis	12.51	12.34	19	42720	3490	32467297
Erythropoiesis abnormal	12.48	12.34	6	42733	214	32470573
Conjunctival haemorrhage	12.44	12.34	17	42722	2838	32467949
Heart rate decreased	12.41	12.34	9	42730	25191	32445596
Skin neoplasm excision	12.35	12.34	7	42732	352	32470435

Pharmacologic Action:

Source	Code	Description
ATC	L01EA01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS BCR-ABL tyrosine kinase inhibitors
FDA MoA	N0000020009	Bcr-Abl Tyrosine Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
CHEBI has role	CHEBI:35610	cytostatic
CHEBI has role	CHEBI:38637	protein tyrosine kinase inhibitor
CHEBI has role	CHEBI:68495	Type I programmed cell-death inducer
CHEBI has role	CHEBI:149553	anti-coronaviral agents

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Dermatofibrosarcoma protuberans	indication	276799004
Systemic mast cell disease	indication	397016004	DOID:349
Blastic phase chronic myeloid leukemia	indication	413656006
Chronic eosinophilic leukemia	indication	413836008
Chronic phase chronic myeloid leukemia	indication	413847001
Gastrointestinal stromal tumor	indication	420120006	DOID:9253
Idiopathic hypereosinophilic syndrome	indication	423294001
Philadelphia chromosome-positive acute lymphoblastic leukemia	indication	425688002
Philadelphia Chromosome Positive Chronic Myelocytic Leukemia	indication	449108003
Myelodysplastic/myeloproliferative diseases with re-arrangements of the gene for platelet-derived growth factor receptor (PDGFR)	indication	738527001
Chronic Myelocytic Leukemia Accelerated Phase	indication
Heart valve disorder	contraindication	368009	DOID:4079
Cerebral edema	contraindication	2032001
Hypophosphatemia	contraindication	4996001
Congenital heart disease	contraindication	13213009
Hyperbilirubinemia	contraindication	14783006	DOID:2741
Pulmonary edema	contraindication	19242006	DOID:11396
Hypertensive disorder	contraindication	38341003	DOID:10763
Body fluid retention	contraindication	43498006
Chronic heart failure	contraindication	48447003
Myocarditis	contraindication	50920009	DOID:820
Gastrointestinal perforation	contraindication	51875005
Hepatic failure	contraindication	59927004
Diabetes mellitus	contraindication	73211009	DOID:9351
Gastrointestinal hemorrhage	contraindication	74474003
Left heart failure	contraindication	85232009
Cardiogenic shock	contraindication	89138009
Kidney disease	contraindication	90708001	DOID:557
Bleeding	contraindication	131148009
Liver function tests abnormal	contraindication	166603001
Disease of liver	contraindication	235856003	DOID:409
Edema	contraindication	267038008
Anemia	contraindication	271737000	DOID:2355
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Neutropenic disorder	contraindication	303011007	DOID:1227
Pericardial effusion	contraindication	373945007	DOID:118
Purpuric disorder	contraindication	387778001
Ascites	contraindication	389026000
Breastfeeding (mother)	contraindication	413712001
Disorder of coronary artery	contraindication	414024009
Obesity	contraindication	414916001	DOID:9970
Pleural Effusions	contraindication
Chronic Heart Failure Following Myocardial Infarction	contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.96	acidic
pKa2	8.49	Basic
pKa3	4.34	Basic
pKa4	3.73	Basic
pKa5	2.2	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	Kd	7.89		CHEMBL	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	Kd	7.85		CHEMBL	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN	INHIBITOR	Kd	8.96		CHEMBL	CHEMBL
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.71		DRUG MATRIX
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		Ki	7.52		CHEMBL
Multidrug resistance-associated protein 1	Transporter	P33527	MRP1_HUMAN					WOMBAT-PK
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.47		CHEMBL
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN		Ki	7.50		CHEMBL
Carbonic anhydrase 4	Enzyme	P22748	CAH4_HUMAN		Ki	5.34		CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		IC50	6.40		CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	7.12		CHEMBL
Carbonic anhydrase 12	Enzyme	O43570	CAH12_HUMAN		Ki	6.01		CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	5.12		CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	4.69		CHEMBL
Carbonic anhydrase 5B, mitochondrial	Enzyme	Q9Y2D0	CAH5B_HUMAN		Ki	4.77		CHEMBL
Carbonic anhydrase 7	Enzyme	P43166	CAH7_HUMAN		Ki	6.96		CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Ki	4.51		CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	7.40		CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	5.51		CHEMBL
RAF proto-oncogene serine/threonine-protein kinase	Kinase	P04049	RAF1_HUMAN		Kd	5.77		CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		Kd	5.48		CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	5.20		CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN		IC50	4.59		CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		Kd	7.96		CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		Kd	7.51		CHEMBL
Insulin receptor	Kinase	P06213	INSR_HUMAN	AGONIST	Ki	5		PDSP
Thromboxane-A synthase	Enzyme	P24557	THAS_HUMAN		IC50	6.70		DRUG MATRIX
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	5.49		CHEMBL
Carbonic anhydrase 3	Enzyme	P07451	CAH3_HUMAN		Ki	6.28		CHEMBL
Carbonic anhydrase 6	Enzyme	P23280	CAH6_HUMAN		Ki	6.41		CHEMBL
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	5.51		CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Ki	5		PDSP
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		IC50	5.30		CHEMBL
Ephrin type-A receptor 8	Kinase	P29322	EPHA8_HUMAN		Kd	5.85		CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	6.05		CHEMBL
Cytoplasmic tyrosine-protein kinase BMX	Kinase	P51813	BMX_HUMAN		Ki	5		PDSP
Carbonic anhydrase 14	Enzyme	Q9ULX7	CAH14_HUMAN		Ki	6.33		CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN		Ki	5		PDSP
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	5.11		CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	8.22		CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		Ki	5		PDSP
Serine/threonine-protein kinase 17A	Kinase	Q9UEE5	ST17A_HUMAN		Kd	5.55		CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	5.62		CHEMBL
Mitogen-activated protein kinase 14	Kinase	Q16539	MK14_HUMAN		IC50	4.86		CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	5.82		CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	5.35		CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	6		CHEMBL
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		Ki	5		PDSP
Dual specificity protein kinase CLK4	Kinase	Q9HAZ1	CLK4_HUMAN		Kd	5.68		CHEMBL
Mitogen-activated protein kinase 9	Kinase	P45984	MK09_HUMAN		Kd	5.28		CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	9.15		CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Ki	5		PDSP
Lysine--tRNA ligase	Enzyme	Q15046	SYK_HUMAN		Ki	5.30		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	5.06		CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	5.59		CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	5.42		CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	5.72		CHEMBL
Serine/threonine-protein kinase TNNI3K	Kinase	Q59H18	TNI3K_HUMAN		Kd	5.37		CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	7.82		CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	6.28		CHEMBL
Cyclin-dependent kinase 19	Kinase	Q9BWU1	CDK19_HUMAN		Kd	5.26		CHEMBL
Homeodomain-interacting protein kinase 4	Kinase	Q8NE63	HIPK4_HUMAN		Kd	6.02		CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	5.92		CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma	Kinase	Q8TBX8	PI42C_HUMAN		Kd	6.42		CHEMBL
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	5.38		CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	7.40		CHEMBL
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	6.46		CHEMBL
Solute carrier family 22 member 3	Transporter	O75751	S22A3_HUMAN		IC50	4.59		CHEMBL
Platelet-derived growth factor receptor	Kinase	P09619 P16234	PGFRB_HUMAN PGFRA_HUMAN		IC50	7.30		CHEMBL
Tyrosine-protein kinase ABL	Kinase	P00519 P42684	ABL1_HUMAN ABL2_HUMAN		IC50	7.40		CHEMBL
Bcr/Abl fusion protein	Kinase	P00519 P11274	ABL1_HUMAN BCR_HUMAN		Ki	7.85		CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	5.14		CHEMBL
ATP-dependent RNA helicase DDX3X	Enzyme	O00571	DDX3X_HUMAN		Kd	6.36		CHEMBL
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	6.13		DRUG MATRIX
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.27		DRUG MATRIX
Carbonic anhydrase 13	Enzyme		CAH13_MOUSE		Ki	5.13		CHEMBL
Carbonic anhydrase 15	Enzyme		CAH15_MOUSE		Ki	7.11		CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase		SRC_CHICK		IC50	5.56		CHEMBL
Tyrosine-protein kinase ABL1	Kinase		ABL1_MOUSE		IC50	7.97		CHEMBL
Platelet-derived growth factor receptor beta	Kinase		PGFRB_RAT		IC50	6.79		CHEMBL

External reference:

ID	Source
4021257	VUID
N0000148698	NUI
D01441	KEGG_DRUG
220127-57-1	SECONDARY_CAS_RN
4021257	VANDF
4021258	VANDF
C0939537	UMLSCUI
CHEBI:45783	CHEBI
STI	PDB_CHEM_ID
CHEMBL941	ChEMBL_ID
CHEMBL1642	ChEMBL_ID
D000068877	MESH_DESCRIPTOR_UI
DB00619	DRUGBANK_ID
5687	IUPHAR_LIGAND_ID
8031	INN_ID
BKJ8M8G5HI	UNII
5291	PUBCHEM_CID
282386	RXNORM
16030	MMSL
238904	MMSL
41395	MMSL
d04758	MMSL
009151	NDDF
009152	NDDF
129558005	SNOMEDCT_US
391634008	SNOMEDCT_US
414460008	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0248	TABLET, FILM COATED	100 mg	ORAL	ANDA	26 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0249	TABLET, FILM COATED	400 mg	ORAL	ANDA	26 sections
Gleevec	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0401	TABLET	100 mg	ORAL	NDA	32 sections
Gleevec	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0649	TABLET	400 mg	ORAL	NDA	32 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7629	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7630	TABLET, FILM COATED	400 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-2245	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-2246	TABLET, FILM COATED	400 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6621	TABLET, FILM COATED	400 mg	ORAL	ANDA	26 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6901	TABLET, FILM COATED	100 mg	ORAL	ANDA	26 sections
imatinib mesylate	Human Prescription Drug Label	1	16714-704	TABLET, FILM COATED	100 mg	ORAL	ANDA	29 sections
imatinib mesylate	Human Prescription Drug Label	1	16714-705	TABLET, FILM COATED	400 mg	ORAL	ANDA	29 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	42292-043	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	42292-044	TABLET, FILM COATED	400 mg	ORAL	ANDA	28 sections
Imatinib	HUMAN PRESCRIPTION DRUG LABEL	1	43598-344	TABLET	100 mg	ORAL	ANDA	26 sections
Imatinib	HUMAN PRESCRIPTION DRUG LABEL	1	43598-345	TABLET	400 mg	ORAL	ANDA	26 sections
imatinib mesylate	Human Prescription Drug Label	1	47335-472	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
imatinib mesylate	Human Prescription Drug Label	1	47335-475	TABLET, FILM COATED	400 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	50268-426	TABLET, FILM COATED	100 mg	ORAL	ANDA	26 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	50268-427	TABLET, FILM COATED	400 mg	ORAL	ANDA	26 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	51407-269	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	51407-270	TABLET, FILM COATED	400 mg	ORAL	ANDA	28 sections
IMATINIB MESYLATE	HUMAN PRESCRIPTION DRUG LABEL	1	51991-376	TABLET, COATED	100 mg	ORAL	ANDA	33 sections
IMATINIB MESYLATE	HUMAN PRESCRIPTION DRUG LABEL	1	51991-377	TABLET, COATED	400 mg	ORAL	ANDA	33 sections
Imatinib Mesylate	Human Prescription Drug Label	1	59651-240	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	Human Prescription Drug Label	1	59651-241	TABLET, FILM COATED	400 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	59923-723	TABLET, COATED	100 mg	ORAL	ANDA	32 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	59923-724	TABLET, COATED	400 mg	ORAL	ANDA	32 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60505-2900	TABLET, FILM COATED	100 mg	ORAL	ANDA	26 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60505-2901	TABLET, FILM COATED	400 mg	ORAL	ANDA	26 sections