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:

None

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
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	1435.05	12.83	1542	36073	334006	46314441
Gastrointestinal stromal tumour	792.56	12.83	184	37431	956	46647491
Chronic myeloid leukaemia	753.32	12.83	206	37409	2252	46646195
Blast crisis in myelogenous leukaemia	625.31	12.83	131	37484	377	46648070
Cytogenetic analysis abnormal	497.60	12.83	111	37504	465	46647982
Drug resistance	442.58	12.83	235	37380	17133	46631314
Second primary malignancy	404.37	12.83	164	37451	6420	46642027
Malignant neoplasm progression	395.75	12.83	364	37251	64562	46583885
Periorbital oedema	277.20	12.83	116	37499	4919	46643528
Gene mutation identification test positive	243.48	12.83	49	37566	107	46648340
Neoplasm malignant	220.17	12.83	169	37446	23330	46625117
Philadelphia chromosome positive	190.62	12.83	45	37570	254	46648193
Chromosome analysis abnormal	181.18	12.83	38	37577	110	46648337
Leukaemia recurrent	175.52	12.83	58	37557	1251	46647196
Chronic myeloid leukaemia recurrent	163.24	12.83	37	37578	169	46648278
Muscle spasms	161.77	12.83	326	37289	122787	46525660
Rheumatoid arthritis	157.38	12.83	9	37606	240206	46408241
Oedema	156.13	12.83	229	37386	66842	46581605
Acute lymphocytic leukaemia recurrent	155.98	12.83	60	37555	2035	46646412
Pleural effusion	155.11	12.83	256	37359	82696	46565751
Chronic myeloid leukaemia transformation	141.74	12.83	30	37585	92	46648355
Gastric antral vascular ectasia	138.34	12.83	40	37575	542	46647905
Eye swelling	130.68	12.83	117	37498	19986	46628461
Eyelid oedema	118.39	12.83	84	37531	10273	46638174
Bone marrow failure	107.48	12.83	126	37489	29543	46618904
Fluid retention	105.56	12.83	165	37450	50881	46597566
Completed suicide	93.88	12.83	6	37609	145914	46502533
Drug hypersensitivity	91.53	12.83	41	37574	243784	46404663
Pancytopenia	90.61	12.83	207	37408	84851	46563596
Rash	88.33	12.83	539	37076	355973	46292474
Face oedema	87.76	12.83	92	37523	19061	46629386
Conjunctival haemorrhage	86.38	12.83	44	37571	2937	46645510
Nausea	82.74	12.83	880	36735	686574	45961873
Oedema peripheral	82.17	12.83	299	37316	159407	46489040
Gene mutation	80.65	12.83	31	37584	1049	46647398
Pseudoporphyria	79.02	12.83	20	37595	157	46648290
Normal newborn	78.77	12.83	53	37562	5948	46642499
Anaemia	77.98	12.83	409	37206	255370	46393077
Product substitution issue	77.60	12.83	77	37538	14954	46633493
Blast cell crisis	75.86	12.83	16	37599	48	46648399
Metastases to liver	75.67	12.83	86	37529	19499	46628948
Growth retardation	73.42	12.83	28	37587	927	46647520
Cytogenetic abnormality	72.78	12.83	24	37591	514	46647933
Graft versus host disease	72.00	12.83	52	37563	6536	46641911
Generalised oedema	71.09	12.83	72	37543	14327	46634120
Thrombocytosis	67.63	12.83	45	37570	4957	46643490
Swelling face	66.59	12.83	138	37477	52921	46595526
Acute lymphocytic leukaemia	66.32	12.83	36	37579	2737	46645710
Recurrent cancer	66.07	12.83	31	37584	1728	46646719
Off label use	66.02	12.83	129	37486	379712	46268735
Exposure via father	65.46	12.83	20	37595	331	46648116
Disease progression	63.09	12.83	189	37426	91111	46557336
Haematotoxicity	60.86	12.83	48	37567	6885	46641562
Hepatotoxicity	60.47	12.83	87	37528	24922	46623525
Chronic graft versus host disease	58.64	12.83	33	37582	2692	46645755
Splenomegaly	58.28	12.83	54	37561	9634	46638813
Hypotension	58.15	12.83	61	37554	232528	46415919
Fall	57.82	12.83	111	37504	328986	46319461
Polymerase chain reaction positive	56.17	12.83	12	37603	39	46648408
Thrombocytopenia	55.22	12.83	225	37390	126356	46522091
Neoplasm progression	54.78	12.83	86	37529	26597	46621850
Pain	52.82	12.83	202	37413	476746	46171701
Bone pain	51.99	12.83	116	37499	46774	46601673
Neoplasm recurrence	51.78	12.83	29	37586	2344	46646103
Pericardial effusion	50.61	12.83	81	37534	25462	46622985
Arthropathy	50.23	12.83	5	37610	84695	46563752
Therapy non-responder	49.26	12.83	105	37510	41047	46607400
Therapeutic response decreased	48.13	12.83	107	37508	43038	46605409
Leukaemia	47.85	12.83	31	37584	3264	46645183
Drug intolerance	47.39	12.83	239	37376	146810	46501637
Exposure via body fluid	47.23	12.83	17	37598	477	46647970
Vomiting	46.62	12.83	563	37052	452231	46196216
Metastases to peritoneum	46.23	12.83	28	37587	2620	46645827
Eye haemorrhage	45.73	12.83	41	37574	7011	46641436
Urinary tract infection	44.40	12.83	68	37547	220198	46428249
Cardiac output decreased	43.54	12.83	19	37596	893	46647554
Chordoma	42.87	12.83	7	37608	0	46648447
Haemoglobin decreased	42.54	12.83	211	37404	128738	46519709
Eye oedema	41.61	12.83	21	37594	1374	46647073
Psoriasis	40.96	12.83	7	37608	78597	46569850
Overdose	40.05	12.83	16	37599	101963	46546484
Diarrhoea	39.54	12.83	651	36964	558951	46089496
Platelet count increased	39.30	12.83	54	37561	14820	46633627
White blood cell count increased	38.89	12.83	100	37515	44119	46604328
Confusional state	37.65	12.83	44	37571	159848	46488599
Erythrocyanosis	36.75	12.83	6	37609	0	46648447
Blast cells present	36.34	12.83	13	37602	358	46648089
Therapeutic product effect decreased	35.79	12.83	11	37604	82590	46565857
Chloroma	35.78	12.83	11	37604	186	46648261
Neutropenia	35.59	12.83	217	37398	142987	46505460
Therapeutic response delayed	34.81	12.83	14	37601	535	46647912
Exposure via partner	34.41	12.83	10	37605	138	46648309
Skin fragility	33.86	12.83	14	37601	575	46647872
Myalgia	33.47	12.83	191	37424	122897	46525550
Tumour excision	33.36	12.83	12	37603	336	46648111
Platelet count decreased	33.20	12.83	164	37451	99860	46548587
Condition aggravated	33.08	12.83	95	37520	244957	46403490
Acute kidney injury	32.90	12.83	90	37525	235765	46412682
Ascites	32.44	12.83	83	37532	36501	46611946
Sinusitis	32.43	12.83	34	37581	129734	46518713
Bone marrow oedema	32.14	12.83	15	37600	826	46647621
Bone marrow transplant	32.12	12.83	14	37601	656	46647791
Myelofibrosis	31.94	12.83	17	37598	1242	46647205
Pneumatosis intestinalis	31.76	12.83	20	37595	2005	46646442
White blood cell count decreased	31.73	12.83	176	37439	112055	46536392
Systemic lupus erythematosus	31.44	12.83	7	37608	65173	46583274
Pulse waveform abnormal	30.64	12.83	8	37607	72	46648375
Trisomy 8	30.62	12.83	5	37610	0	46648447
Ankle brachial index decreased	30.54	12.83	8	37607	73	46648374
Carotid intima-media thickness increased	30.06	12.83	8	37607	78	46648369
Leukocytosis	29.51	12.83	61	37554	23337	46625110
Intentional overdose	29.33	12.83	8	37607	64936	46583511
Asthma	29.03	12.83	19	37596	91523	46556924
Blood lactate dehydrogenase increased	28.91	12.83	56	37559	20444	46628003
Cardiotoxicity	28.51	12.83	31	37584	6691	46641756
Pyrexia	28.44	12.83	416	37199	348386	46300061
Breast cancer	28.41	12.83	91	37524	45427	46603020
Toxic skin eruption	28.35	12.83	42	37573	12345	46636102
Jaundice	28.27	12.83	68	37547	28777	46619670
Loss of personal independence in daily activities	27.86	12.83	6	37609	57177	46591270
Right ventricular failure	27.81	12.83	48	37567	16045	46632402
Typhoid fever	27.74	12.83	6	37609	21	46648426
Gastrointestinal toxicity	27.72	12.83	25	37590	4306	46644141
Aplasia	27.66	12.83	23	37592	3553	46644894
Morphoea	27.31	12.83	10	37605	295	46648152
Dizziness	27.14	12.83	162	37453	340252	46308195
Left ventricular dysfunction	26.74	12.83	37	37578	10218	46638229
Syncope	26.70	12.83	27	37588	104776	46543671
Blast cell count increased	25.67	12.83	10	37605	351	46648096
Surgery	25.20	12.83	65	37550	28720	46619727
Anxiety	24.94	12.83	70	37545	181887	46466560
Tumour haemorrhage	24.80	12.83	15	37600	1400	46647047
Somnolence	24.71	12.83	56	37559	156465	46491982
Transdifferentiation of neoplasm	24.51	12.83	5	37610	12	46648435
Pubertal failure	24.51	12.83	5	37610	12	46648435
Peritoneal lesion	24.50	12.83	4	37611	0	46648447
Slit-lamp tests abnormal	24.50	12.83	4	37611	0	46648447
Lower respiratory tract infection	24.48	12.83	7	37608	55082	46593365
Inappropriate schedule of product administration	24.24	12.83	11	37604	65002	46583445
Back pain	23.77	12.83	88	37527	209951	46438496
Blood pressure increased	23.72	12.83	41	37574	126625	46521822
Urine odour abnormal	23.02	12.83	24	37591	4938	46643509
Agitation	22.91	12.83	8	37607	55407	46593040
Abortion	22.87	12.83	17	37598	2233	46646214
Hallucination	22.84	12.83	6	37609	49945	46598502
Nasopharyngitis	22.80	12.83	57	37558	153941	46494506
Injury	22.76	12.83	4	37611	44023	46604424
Peripheral arterial occlusive disease	22.73	12.83	21	37594	3731	46644716
Hyponatraemia	22.66	12.83	29	37586	101303	46547144
Hepatic necrosis	22.32	12.83	25	37590	5576	46642871
Suicidal ideation	21.88	12.83	9	37606	56373	46592074
Cytopenia	21.73	12.83	29	37586	7739	46640708
Papilloedema	21.63	12.83	20	37595	3557	46644890
Exposure during pregnancy	21.43	12.83	155	37460	108057	46540390
Blood test abnormal	21.39	12.83	32	37583	9488	46638959
Leukopenia	21.22	12.83	110	37505	68233	46580214
Tumour necrosis	21.18	12.83	11	37604	764	46647683
Abortion spontaneous	20.95	12.83	80	37535	43566	46604881
Gastric cancer	20.94	12.83	18	37597	2911	46645536
Basophilia	20.84	12.83	4	37611	6	46648441
Periorbital swelling	20.81	12.83	13	37602	1285	46647162
Chylothorax	20.80	12.83	8	37607	271	46648176
Lacrimation increased	20.76	12.83	42	37573	15819	46632628
Joint swelling	20.52	12.83	67	37548	166006	46482441
Chronic graft versus host disease in skin	20.44	12.83	10	37605	612	46647835
Tremor	20.25	12.83	39	37576	115600	46532847
Product use issue	20.23	12.83	28	37587	94616	46553831
Intracardiac mass	20.13	12.83	5	37610	36	46648411
Oral pigmentation	20.11	12.83	4	37611	8	46648439
Drug ineffective	20.02	12.83	406	37209	677432	45971015
Blister	19.96	12.83	80	37535	44551	46603896
Musculoskeletal stiffness	19.96	12.83	30	37585	97963	46550484
Anaphylactic reaction	19.78	12.83	9	37606	53103	46595344
Flushing	19.69	12.83	14	37601	64600	46583847
Arthritis	19.60	12.83	20	37595	77296	46571151
Stem cell transplant	19.43	12.83	14	37601	1752	46646695
Loss of consciousness	19.39	12.83	36	37579	108202	46540245
Swelling of eyelid	19.28	12.83	12	37603	1179	46647268
Computerised tomogram abnormal	18.93	12.83	15	37600	2165	46646282
Acute myeloid leukaemia	18.57	12.83	40	37575	15738	46632709
Neoplasm	18.37	12.83	23	37592	5765	46642682
Influenza like illness	18.18	12.83	12	37603	57558	46590889
Myelocytosis	18.07	12.83	4	37611	16	46648431
Insomnia	18.07	12.83	70	37545	164854	46483593
Cellulitis	18.02	12.83	18	37597	70270	46578177
Urticaria	17.94	12.83	43	37572	117849	46530598
Pulmonary embolism	17.83	12.83	38	37577	108547	46539900
Aspiration pleural cavity	17.82	12.83	10	37605	811	46647636
Headache	17.75	12.83	275	37340	478077	46170370
Deep vein thrombosis	17.66	12.83	23	37592	79750	46568697
Liver disorder	17.65	12.83	68	37547	37178	46611269
Dengue fever	17.52	12.83	9	37606	611	46647836
Ejection fraction decreased	17.27	12.83	42	37573	17895	46630552
Pigmentation disorder	17.22	12.83	18	37597	3715	46644732
Obliterative bronchiolitis	17.13	12.83	13	37602	1762	46646685
Scleroderma-like reaction	17.01	12.83	5	37610	72	46648375
Hypertension	16.94	12.83	91	37524	196265	46452182
Product dose omission issue	16.91	12.83	74	37541	168446	46480001
Hyperkalaemia	16.79	12.83	10	37605	50699	46597748
Lichen planus	16.75	12.83	13	37602	1820	46646627
Disseminated intravascular coagulation	16.72	12.83	43	37572	18962	46629485
Hyperhidrosis	16.63	12.83	29	37586	89279	46559168
Eosinophilia	16.42	12.83	43	37572	19174	46629273
Seizure	16.36	12.83	48	37567	123006	46525441
Fibrin degradation products increased	16.35	12.83	6	37609	178	46648269
Gastrointestinal angiectasia	16.19	12.83	5	37610	86	46648361
Acute graft versus host disease	16.08	12.83	18	37597	4012	46644435
Intentional product misuse	16.03	12.83	9	37606	47119	46601328
Lichenoid keratosis	15.82	12.83	11	37604	1302	46647145
Tumour lysis syndrome	15.80	12.83	24	37591	7212	46641235
Central nervous system leukaemia	15.77	12.83	5	37610	94	46648353
Abortion induced	15.67	12.83	29	37586	10231	46638216
Blood blister	15.62	12.83	12	37603	1656	46646791
Skin hypopigmentation	15.58	12.83	7	37608	353	46648094
Fibromyalgia	15.53	12.83	5	37610	36458	46611989
Therapy partial responder	15.49	12.83	19	37596	4663	46643784
Jaw operation	15.43	12.83	9	37606	786	46647661
Intentional product use issue	15.36	12.83	12	37603	52768	46595679
Metastasis	15.09	12.83	18	37597	4294	46644153
Growth disorder	15.08	12.83	3	37612	6	46648441
Hair colour changes	14.86	12.83	12	37603	1780	46646667
Acute leukaemia	14.81	12.83	10	37605	1128	46647319
Wound	14.81	12.83	8	37607	42794	46605653
Subdural haematoma evacuation	14.77	12.83	3	37612	7	46648440
Therapy interrupted	14.63	12.83	29	37586	10762	46637685
Therapy cessation	14.63	12.83	51	37564	26578	46621869
Cardio-respiratory arrest	14.59	12.83	16	37599	59853	46588594
Hepatic neoplasm	14.56	12.83	12	37603	1832	46646615
Delirium	14.35	12.83	6	37609	37222	46611225
Glossodynia	14.35	12.83	9	37606	44364	46604083
Suicide attempt	14.21	12.83	14	37601	55022	46593425
Vascular malformation	14.21	12.83	5	37610	131	46648316
Irritability	14.18	12.83	3	37612	28943	46619504
Dry skin	14.13	12.83	68	37547	40948	46607499
Primary adrenal insufficiency	13.98	12.83	4	37611	52	46648395
Mobility decreased	13.90	12.83	17	37598	60577	46587870
Gastrectomy	13.84	12.83	7	37608	460	46647987
Osteoarthritis	13.61	12.83	18	37597	62007	46586440
Myeloid maturation arrest	13.56	12.83	3	37612	12	46648435
Dermatofibrosarcoma protuberans	13.56	12.83	3	37612	12	46648435
Leukaemic infiltration extramedullary	13.46	12.83	4	37611	60	46648387
Polymerase chain reaction	13.36	12.83	3	37612	13	46648434
Myelosuppression	13.34	12.83	23	37592	7680	46640767
Toxicity to various agents	13.28	12.83	108	37507	211658	46436789
Adenocarcinoma gastric	13.17	12.83	7	37608	510	46647937
Parakeratosis	13.15	12.83	5	37610	164	46648283
Drug withdrawal syndrome	13.08	12.83	3	37612	27381	46621066
Cystitis	13.07	12.83	9	37606	42232	46606215
Acute myeloid leukaemia recurrent	12.98	12.83	10	37605	1386	46647061
Desmoid tumour	12.88	12.83	4	37611	70	46648377

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	2275.57	11.83	2561	37437	354722	29557758
Gastrointestinal stromal tumour	1139.64	11.83	279	39719	1027	29911453
Chronic myeloid leukaemia	982.60	11.83	286	39712	2291	29910189
Drug resistance	746.76	11.83	414	39584	19719	29892761
Blast crisis in myelogenous leukaemia	712.58	11.83	161	39837	373	29912107
Second primary malignancy	588.04	11.83	245	39753	6111	29906369
Malignant neoplasm progression	454.45	11.83	520	39478	71767	29840713
Neoplasm malignant	371.96	11.83	254	39744	17560	29894920
Cytogenetic analysis abnormal	328.00	11.83	82	39916	335	29912145
Philadelphia chromosome positive	277.80	11.83	64	39934	167	29912313
Pleural effusion	200.98	11.83	357	39641	73709	29838771
Gene mutation	193.37	11.83	63	39935	758	29911722
Chromosome analysis abnormal	186.85	11.83	41	39957	78	29912402
Metastases to liver	158.66	11.83	130	39868	11835	29900645
Leukaemia recurrent	157.29	11.83	64	39934	1497	29910983
Drug intolerance	155.85	11.83	243	39755	45048	29867432
Chronic myeloid leukaemia recurrent	154.88	11.83	36	39962	99	29912381
Chronic myeloid leukaemia transformation	150.02	11.83	37	39961	141	29912339
Acute lymphocytic leukaemia recurrent	148.09	11.83	72	39926	2595	29909885
Periorbital oedema	144.33	11.83	76	39922	3250	29909230
Gene mutation identification test positive	122.23	11.83	32	39966	163	29912317
Recurrent cancer	110.95	11.83	46	39952	1130	29911350
Therapeutic response decreased	104.45	11.83	145	39853	24204	29888276
Blast cell crisis	98.49	11.83	23	39975	65	29912415
Muscle spasms	96.74	11.83	245	39753	64593	29847887
Hypotension	95.30	11.83	77	39921	200488	29711992
Oedema	95.02	11.83	190	39808	42803	29869677
Drug abuse	92.50	11.83	4	39994	82068	29830412
Completed suicide	92.19	11.83	12	39986	99480	29813000
Eyelid oedema	91.40	11.83	66	39932	4979	29907501
Chronic graft versus host disease	88.91	11.83	60	39938	4059	29908421
Neoplasm recurrence	87.71	11.83	45	39953	1822	29910658
Acute kidney injury	84.41	11.83	148	39850	273694	29638786
White blood cell count increased	83.70	11.83	172	39826	39501	29872979
Neoplasm progression	82.84	11.83	111	39887	17912	29894568
Overdose	78.54	11.83	10	39988	84327	29828153
Gastric antral vascular ectasia	76.93	11.83	25	39973	298	29912182
Desmoid tumour	74.24	11.83	19	39979	87	29912393
Therapy non-responder	70.94	11.83	135	39863	29318	29883162
Polymerase chain reaction positive	70.77	11.83	18	39980	80	29912400
Face oedema	65.08	11.83	78	39920	11256	29901224
Splenomegaly	65.00	11.83	85	39913	13395	29899085
Necrotising panniculitis	63.34	11.83	14	39984	28	29912452
Prostate cancer	62.94	11.83	114	39884	23843	29888637
Chordoma	61.82	11.83	11	39987	0	29912480
Clonal evolution	61.77	11.83	17	39981	108	29912372
Graft versus host disease	60.17	11.83	71	39927	10079	29902401
Fluid retention	58.25	11.83	113	39885	24885	29887595
Metastases to peritoneum	57.57	11.83	32	39966	1525	29910955
Acquired gene mutation	57.50	11.83	29	39969	1132	29911348
Scleroderma	56.65	11.83	30	39968	1297	29911183
Fall	54.39	11.83	100	39898	181772	29730708
Blast cell count increased	54.30	11.83	27	39971	1022	29911458
Toxicity to various agents	54.26	11.83	96	39902	177087	29735393
Central nervous system leukaemia	53.15	11.83	18	39980	246	29912234
Acute lymphocytic leukaemia	52.95	11.83	39	39959	3033	29909447
Product substitution issue	51.08	11.83	65	39933	9970	29902510
Off label use	51.04	11.83	167	39831	249123	29663357
Bradycardia	49.78	11.83	13	39985	65513	29846967
Bone pain	49.29	11.83	90	39908	18936	29893544
Myelofibrosis	49.27	11.83	29	39969	1542	29910938
Cytogenetic abnormality	48.84	11.83	23	39975	771	29911709
Blast cells present	47.92	11.83	15	39983	157	29912323
Disease progression	47.56	11.83	222	39776	79652	29832828
Accident	47.34	11.83	39	39959	3574	29908906
Confusional state	46.98	11.83	67	39931	134767	29777713
Pituitary apoplexy	46.29	11.83	10	39988	17	29912463
Ascites	45.68	11.83	128	39870	35793	29876687
Typhoid fever	44.91	11.83	10	39988	21	29912459
Endocarditis noninfective	43.89	11.83	13	39985	111	29912369
Bone marrow failure	42.76	11.83	111	39887	29674	29882806
Exposure via father	42.61	11.83	13	39985	124	29912356
Chronic graft versus host disease in skin	41.67	11.83	20	39978	700	29911780
Bone marrow necrosis	41.62	11.83	13	39985	135	29912345
Hyperkalaemia	41.61	11.83	18	39980	65992	29846488
Treatment failure	41.59	11.83	121	39877	34558	29877922
Tumour haemorrhage	41.12	11.83	31	39967	2497	29909983
Intentional overdose	40.91	11.83	4	39994	41477	29871003
Tumour rupture	39.77	11.83	13	39985	158	29912322
Surgery	39.70	11.83	62	39936	11489	29900991
Haemoglobin decreased	38.76	11.83	273	39725	113825	29798655
Loss of therapeutic response	37.55	11.83	11	39987	90	29912390
Somnolence	36.84	11.83	45	39953	96718	29815762
Pulmonary embolism	35.78	11.83	31	39967	78104	29834376
Hallucination	34.92	11.83	11	39987	49048	29863432
Platelet count decreased	34.92	11.83	252	39746	105877	29806603
Colon cancer	34.61	11.83	49	39949	8323	29904157
Drug hypersensitivity	34.12	11.83	25	39973	68494	29843986
Tumour necrosis	33.82	11.83	20	39978	1073	29911407
Gastrectomy	33.41	11.83	11	39987	137	29912343
Gastric cancer	33.35	11.83	37	39961	4913	29907567
Nausea	32.65	11.83	567	39431	296390	29616090
Cardiac arrest	32.46	11.83	46	39952	92804	29819676
Drug interaction	32.22	11.83	147	39851	199421	29713059
Eye swelling	32.05	11.83	49	39949	8915	29903565
Generalised oedema	31.77	11.83	57	39941	11828	29900652
Growth retardation	31.44	11.83	22	39976	1578	29910902
Seizure	31.34	11.83	52	39946	98423	29814057
Pulmonary aplasia	31.29	11.83	6	39992	3	29912477
Pneumonia	31.20	11.83	291	39707	334015	29578465
Tumour excision	31.10	11.83	10	39988	115	29912365
Thrombocytopenia	30.96	11.83	299	39699	136745	29775735
Chloroma	30.80	11.83	14	39984	432	29912048
Syncope	30.74	11.83	41	39957	84862	29827618
Oral pigmentation	29.57	11.83	6	39992	6	29912474
Rhabdomyolysis	29.38	11.83	25	39973	63555	29848925
Delirium	29.12	11.83	9	39989	40622	29871858
Pericardial effusion	28.51	11.83	77	39921	21067	29891413
Malaria	28.17	11.83	11	39987	230	29912250
Renal tuberculosis	28.10	11.83	5	39993	0	29912480
Stem cell transplant	27.91	11.83	23	39975	2108	29910372
Deep vein thrombosis	27.70	11.83	24	39974	60477	29852003
Anxiety	27.18	11.83	49	39949	89822	29822658
Pseudoporphyria	27.04	11.83	11	39987	257	29912223
Blindness	26.68	11.83	54	39944	12255	29900225
Inappropriate schedule of product administration	26.39	11.83	10	39988	39718	29872762
Flushing	26.25	11.83	4	39994	29488	29882992
Psoriasis	26.14	11.83	12	39986	42494	29869986
Dizziness	26.13	11.83	153	39845	194756	29717724
Hyperhidrosis	25.74	11.83	31	39967	67059	29845421
Demyelination	25.72	11.83	24	39974	2596	29909884
Graft versus host disease in eye	25.57	11.83	10	39988	210	29912270
Rash	25.38	11.83	378	39620	191511	29720969
Optic neuritis	25.00	11.83	26	39972	3208	29909272
Cardio-respiratory arrest	24.73	11.83	24	39974	57282	29855198
Plasma cell myeloma	24.73	11.83	21	39977	53441	29859039
Tremor	24.72	11.83	39	39959	75324	29837156
International normalised ratio increased	24.31	11.83	17	39981	47722	29864758
Metabolic acidosis	23.95	11.83	10	39988	37451	29875029
Oedema peripheral	23.93	11.83	231	39767	105601	29806879
Therapy partial responder	23.85	11.83	27	39971	3664	29908816
Therapeutic product effect decreased	23.59	11.83	5	39993	29071	29883409
Large intestine infection	23.49	11.83	17	39981	1286	29911194
Post embolisation syndrome	23.41	11.83	7	39991	62	29912418
Bone marrow transplant	23.07	11.83	15	39983	953	29911527
Right ventricular diastolic collapse	22.92	11.83	7	39991	67	29912413
Chronic obstructive pulmonary disease	22.74	11.83	17	39981	46109	29866371
Intentional product misuse	22.57	11.83	9	39989	34658	29877822
Spleen palpable	22.48	11.83	4	39994	0	29912480
Acute aortic syndrome	22.48	11.83	4	39994	0	29912480
Philadelphia chromosome negative	22.48	11.83	4	39994	0	29912480
Agitation	21.80	11.83	24	39974	54049	29858431
Pemphigus	21.71	11.83	16	39982	1245	29911235
B-cell small lymphocytic lymphoma	21.70	11.83	8	39990	142	29912338
Tachycardia	21.59	11.83	41	39957	73698	29838782
Ocular myasthenia	21.12	11.83	9	39989	237	29912243
Blood pressure increased	21.05	11.83	40	39958	71888	29840592
Haematotoxicity	21.04	11.83	33	39965	6137	29906343
Rectosigmoid cancer	21.01	11.83	8	39990	156	29912324
Epistaxis	20.83	11.83	24	39974	52957	29859523
Tuberculosis	20.65	11.83	38	39960	8039	29904441
Dehydration	20.51	11.83	90	39908	123449	29789031
Transformation to acute myeloid leukaemia	20.46	11.83	12	39986	634	29911846
Bone marrow oedema	20.43	11.83	11	39987	492	29911988
Anaphylactic reaction	20.41	11.83	6	39992	27976	29884504
Aggression	20.35	11.83	12	39986	36895	29875585
Intestinal congestion	20.25	11.83	4	39994	3	29912477
Complications of transplant surgery	20.12	11.83	11	39987	507	29911973
Multiple-drug resistance	19.84	11.83	22	39976	2919	29909561
Concomitant disease aggravated	19.71	11.83	29	39969	5100	29907380
Condition aggravated	19.66	11.83	106	39892	137760	29774720
Periorbital swelling	19.62	11.83	8	39990	188	29912292
Dengue fever	19.58	11.83	8	39990	189	29912291
Suicidal ideation	19.55	11.83	12	39986	36102	29876378
Leukaemia	19.43	11.83	23	39975	3274	29909206
Pancytopenia	19.39	11.83	186	39812	84866	29827614
Blood lactate dehydrogenase increased	19.29	11.83	66	39932	20535	29891945
Urticaria	19.12	11.83	27	39971	54579	29857901
Pericardial excision	18.82	11.83	4	39994	6	29912474
Suicide attempt	18.77	11.83	13	39985	36684	29875796
Drug dependence	18.70	11.83	3	39995	21292	29891188
Neoplasm	18.47	11.83	25	39973	4071	29908409
Marrow hyperplasia	18.34	11.83	13	39985	952	29911528
Dropped head syndrome	18.28	11.83	6	39992	74	29912406
Chest expansion decreased	18.22	11.83	7	39991	140	29912340
Mental status changes	17.85	11.83	14	39984	37065	29875415
Product use in unapproved indication	17.71	11.83	163	39835	73530	29838950
Graft versus host disease in lung	17.51	11.83	10	39988	502	29911978
Bladder cancer	17.48	11.83	38	39960	9064	29903416
Platelet count increased	17.36	11.83	37	39961	8705	29903775
Abscess drainage	17.33	11.83	8	39990	256	29912224
Acinetobacter sepsis	17.28	11.83	5	39993	39	29912441
Gelatinous transformation of the bone marrow	17.21	11.83	4	39994	11	29912469
Pigmentation disorder	16.95	11.83	17	39981	2009	29910471
Janus kinase 2 mutation	16.86	11.83	3	39995	0	29912480
Hepatic embolisation	16.86	11.83	3	39995	0	29912480
Pseudomyxoma peritonei	16.86	11.83	3	39995	0	29912480
Hydrocele operation	16.86	11.83	3	39995	0	29912480
Central nervous system neoplasm	16.85	11.83	5	39993	43	29912437
Therapy change	16.72	11.83	19	39979	2590	29909890
Biopsy bone marrow abnormal	16.61	11.83	8	39990	282	29912198
Blood glucose increased	16.49	11.83	36	39962	61494	29850986
Anaemia	16.37	11.83	378	39620	207614	29704866
Trisomy 8	16.27	11.83	5	39993	49	29912431
Coma	16.25	11.83	18	39980	40431	29872049
Vomiting	16.23	11.83	396	39602	219422	29693058
Medication error	16.23	11.83	4	39994	20968	29891512
Essential thrombocythaemia	16.09	11.83	5	39993	51	29912429
Drug reaction with eosinophilia and systemic symptoms	16.08	11.83	9	39989	28479	29884001
Atrial fibrillation	16.04	11.83	82	39916	108042	29804438
Lactic acidosis	16.04	11.83	11	39987	31202	29881278
Neuropathy peripheral	15.94	11.83	45	39953	70430	29842050
Hyponatraemia	15.88	11.83	42	39956	67160	29845320
Acute myocardial infarction	15.88	11.83	29	39969	52910	29859570
Chills	15.77	11.83	47	39951	72291	29840189
Encephalopathy	15.70	11.83	12	39986	32193	29880287
Disease recurrence	15.63	11.83	48	39950	14113	29898367
Growth failure	15.59	11.83	5	39993	57	29912423
Lung neoplasm malignant	15.52	11.83	50	39948	15082	29897398
Bone marrow disorder	15.47	11.83	14	39984	1456	29911024
Hypereosinophilic syndrome	15.16	11.83	7	39991	224	29912256
Bence Jones proteinuria	14.78	11.83	3	39995	3	29912477
Metastasis	14.67	11.83	20	39978	3278	29909202
Parakeratosis	14.64	11.83	6	39992	143	29912337
Metastases to heart	14.64	11.83	6	39992	143	29912337
Lacrimation increased	14.29	11.83	30	39968	6986	29905494
Hyperchromic anaemia	14.08	11.83	4	39994	29	29912451
Blood pressure decreased	13.93	11.83	26	39972	47049	29865431
Product dose omission issue	13.87	11.83	69	39929	91562	29820918
Insomnia	13.72	11.83	71	39927	93265	29819215
Cellulitis	13.70	11.83	26	39972	46758	29865722
Lymphocytic infiltration	13.68	11.83	9	39989	583	29911897
Ejection fraction decreased	13.67	11.83	48	39950	15127	29897353
Stress	13.59	11.83	5	39993	20230	29892250
Transitional cell carcinoma	13.59	11.83	15	39983	1980	29910500
Laryngeal cancer stage III	13.57	11.83	3	39995	6	29912474
Fibrin D dimer decreased	13.57	11.83	3	39995	6	29912474
Aspiration bone marrow	13.57	11.83	3	39995	6	29912474
Clear cell sarcoma of soft tissue	13.57	11.83	3	39995	6	29912474
Bladder neoplasm surgery	13.32	11.83	4	39994	36	29912444
Wheezing	13.29	11.83	13	39985	30925	29881555
Tumour compression	13.25	11.83	5	39993	95	29912385
Therapy responder	13.23	11.83	6	39992	184	29912296
Colitis	13.19	11.83	13	39985	30807	29881673
Lipase increased	13.13	11.83	33	39965	8643	29903837
Cancer surgery	13.13	11.83	8	39990	453	29912027
Cytopenia	13.13	11.83	32	39966	8224	29904256
Skin neoplasm excision	13.10	11.83	7	39991	308	29912172
Angioedema	13.06	11.83	16	39982	34368	29878112
Erythropoiesis abnormal	13.03	11.83	6	39992	191	29912289
Blast cell proliferation	12.97	11.83	3	39995	8	29912472
Paternal exposure during pregnancy	12.97	11.83	3	39995	8	29912472
Unevaluable event	12.93	11.83	14	39984	31771	29880709
Hyperkeratosis	12.93	11.83	19	39979	3338	29909142
Thrombosis	12.78	11.83	23	39975	42208	29870272
Intentional product use issue	12.77	11.83	18	39980	36422	29876058
Bone development abnormal	12.77	11.83	4	39994	42	29912438
Swelling of eyelid	12.58	11.83	7	39991	334	29912146
Ileus paralytic	12.51	11.83	25	39973	5623	29906857
Breast oedema	12.47	11.83	3	39995	10	29912470
Polycythaemia vera	12.47	11.83	6	39992	211	29912269
Myasthenia gravis crisis	12.41	11.83	7	39991	343	29912137
Arterial intramural haematoma	12.36	11.83	4	39994	47	29912433
Skin depigmentation	12.32	11.83	7	39991	348	29912132
Myositis	12.23	11.83	36	39962	10341	29902139
Leukocytosis	12.22	11.83	59	39939	21443	29891037
Oropharyngeal pain	12.21	11.83	12	39986	28484	29883996
Haemorrhagic ascites	12.20	11.83	5	39993	119	29912361
Hepatotoxicity	11.95	11.83	52	39946	18093	29894387
Constipation	11.93	11.83	95	39903	112811	29799669
Metastases to lymph nodes	11.83	11.83	20	39978	3957	29908523

Pharmacologic Action:

Source	Code	Description
ATC	L01EA01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS BCR-ABL tyrosine kinase inhibitors
FDA MoA	N0000175076	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
CHEBI has role	CHEBI:35610	cytostatic
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
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
Myelodysplastic/ Myeloproliferative Diseases associated with Platelet-derived Growth Factor Receptor	indication
Philadelphia Chromosome Positive Chronic Myelocytic Leukemia	indication
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
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN	INHIBITOR	Kd	8.96		CHEMBL	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	Kd	7.85		CHEMBL	CHEMBL
Ephrin type-B receptor 4	Kinase	P54760	EPHB4_HUMAN		Ki	5		PDSP
Cytoplasmic tyrosine-protein kinase BMX	Kinase	P51813	BMX_HUMAN		Ki	5		PDSP
Insulin receptor	Kinase	P06213	INSR_HUMAN	AGONIST	Ki	5		PDSP
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Ki	5		PDSP
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
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.71		DRUG MATRIX
Thromboxane-A synthase	Enzyme	P24557	THAS_HUMAN		IC50	6.70		DRUG MATRIX
Multidrug resistance-associated protein 1	Transporter	P33527	MRP1_HUMAN					WOMBAT-PK
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	5.51		CHEMBL
Solute carrier family 22 member 3	Transporter	O75751	S22A3_HUMAN		IC50	4.59		CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	5.20		CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	5.12		CHEMBL
Carbonic anhydrase 2	Enzyme	P00918	CAH2_HUMAN		Ki	7.52		CHEMBL
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		IC50	5.14		CHEMBL
Mitogen-activated protein kinase 9	Kinase	P45984	MK09_HUMAN		Kd	5.28		CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN		IC50	4.59		CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Ki	4.51		CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		Kd	7.51		CHEMBL
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	5.38		CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	6		CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	5.59		CHEMBL
Maternal embryonic leucine zipper kinase	Kinase	Q14680	MELK_HUMAN		Kd	5.72		CHEMBL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		IC50	5.30		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
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	5.62		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
Ephrin type-A receptor 8	Kinase	P29322	EPHA8_HUMAN		Kd	5.85		CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	5.11		CHEMBL
Serine/threonine-protein kinase TNNI3K	Kinase	Q59H18	TNI3K_HUMAN		Kd	5.37		CHEMBL
Homeodomain-interacting protein kinase 4	Kinase	Q8NE63	HIPK4_HUMAN		Kd	6.02		CHEMBL
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	6.46		CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	7.40		CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma	Kinase	Q8TBX8	PI42C_HUMAN		Kd	6.42		CHEMBL
Serine/threonine-protein kinase 17A	Kinase	Q9UEE5	ST17A_HUMAN		Kd	5.55		CHEMBL
Dual specificity protein kinase CLK4	Kinase	Q9HAZ1	CLK4_HUMAN		Kd	5.68		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	5.06		CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	5.92		CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	6.05		CHEMBL
Lysine--tRNA ligase	Enzyme	Q15046	SYK_HUMAN		Ki	5.30		CHEMBL
Carbonic anhydrase 12	Enzyme	O43570	CAH12_HUMAN		Ki	6.01		CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	8.22		CHEMBL
Carbonic anhydrase 4	Enzyme	P22748	CAH4_HUMAN		Ki	5.34		CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	6.28		CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	5.49		CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	5.51		CHEMBL
Tyrosine-protein kinase ABL	Kinase	P00519 P42684	ABL1_HUMAN ABL2_HUMAN		IC50	7.40		CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		Kd	7.96		CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	7.82		CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		IC50	6.40		CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	9.15		CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	7.40		CHEMBL
Carbonic anhydrase 3	Enzyme	P07451	CAH3_HUMAN		Ki	6.28		CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	4.69		CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.47		CHEMBL
Carbonic anhydrase 14	Enzyme	Q9ULX7	CAH14_HUMAN		Ki	6.33		CHEMBL
Carbonic anhydrase 7	Enzyme	P43166	CAH7_HUMAN		Ki	6.96		CHEMBL
Bcr/Abl fusion protein	Kinase	P00519 P11274	ABL1_HUMAN BCR_HUMAN		Ki	7.85		CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	7.12		CHEMBL
Cyclin-dependent kinase 19	Kinase	Q9BWU1	CDK19_HUMAN		Kd	5.26		CHEMBL
Carbonic anhydrase 1	Enzyme	P00915	CAH1_HUMAN		Ki	7.50		CHEMBL
Carbonic anhydrase 5B, mitochondrial	Enzyme	Q9Y2D0	CAH5B_HUMAN		Ki	4.77		CHEMBL
Carbonic anhydrase 6	Enzyme	P23280	CAH6_HUMAN		Ki	6.41		CHEMBL
Platelet-derived growth factor receptor	Kinase	P09619 P16234	PGFRA_HUMAN PGFRB_HUMAN		IC50	7.30		CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		Ki	5		PDSP
Mitogen-activated protein kinase 14	Kinase	Q16539	MK14_HUMAN		IC50	4.86		CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN		Ki	5		PDSP
Ephrin type-B receptor 1	Kinase	P54762	EPHB1_HUMAN		Ki	5		PDSP
Carbonic anhydrase 13	Enzyme		CAH13_MOUSE		Ki	5.13		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
Carbonic anhydrase 15	Enzyme		CAH15_MOUSE		Ki	7.11		CHEMBL

External reference:

ID	Source
4021257	VUID
N0000148698	NUI
D01441	KEGG_DRUG
220127-57-1	SECONDARY_CAS_RN
4021257	VANDF
4021258	VANDF
C0385728	UMLSCUI
CHEBI:31690	CHEBI
STI	PDB_CHEM_ID
CHEMBL941	ChEMBL_ID
CHEMBL1642	ChEMBL_ID
DB00619	DRUGBANK_ID
D000068877	MESH_DESCRIPTOR_UI
5291	PUBCHEM_CID
5687	IUPHAR_LIGAND_ID
8031	INN_ID
BKJ8M8G5HI	UNII
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	27 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	42292-044	TABLET, FILM COATED	400 mg	ORAL	ANDA	27 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	60429-925	TABLET, FILM COATED	100 mg	ORAL	ANDA	28 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60429-926	TABLET, FILM COATED	400 mg	ORAL	ANDA	28 sections