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

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
Nausea	905.67	27.31	522	5259	111667	2240637
Death	862.10	27.31	454	5327	81014	2271290
Diarrhoea	700.72	27.31	400	5381	83164	2269140
Chronic myeloid leukaemia	643.81	27.31	119	5662	467	2351837
Rash	638.73	27.31	336	5445	59222	2293082
Malignant neoplasm progression	616.49	27.31	208	5573	11920	2340384
Vomiting	605.00	27.31	345	5436	71257	2281047
Neoplasm malignant	582.73	27.31	163	5618	4930	2347374
Gastrointestinal stromal tumour	573.28	27.31	97	5684	192	2352112
Anaemia	549.59	27.31	256	5525	34536	2317768
Blast crisis in myelogenous leukaemia	545.07	27.31	85	5696	68	2352236
Drug resistance	505.72	27.31	127	5654	2497	2349807
Oedema peripheral	473.81	27.31	206	5575	23557	2328747
Pleural effusion	464.81	27.31	167	5614	11501	2340803
Muscle spasms	452.93	27.31	194	5587	21372	2330932
Fatigue	420.32	27.31	292	5489	84581	2267723
Periorbital oedema	400.90	27.31	88	5693	930	2351374
Dyspnoea	378.01	27.31	266	5515	78467	2273837
Pyrexia	376.10	27.31	230	5551	53478	2298826
Fluid retention	365.81	27.31	123	5658	6923	2345381
Second primary malignancy	363.23	27.31	81	5700	925	2351379
Pancytopenia	342.72	27.31	133	5648	11319	2340985
Oedema	328.52	27.31	125	5656	10078	2342226
Haemoglobin decreased	321.40	27.31	145	5636	18006	2334298
Thrombocytopenia	320.38	27.31	147	5634	18984	2333320
Exposure during pregnancy	284.65	27.31	148	5633	25071	2327233
Eye swelling	281.63	27.31	90	5691	4300	2348004
Gene mutation identification test positive	279.90	27.31	43	5738	27	2352277
Drug intolerance	276.22	27.31	120	5661	13597	2338707
Disease progression	275.61	27.31	128	5653	16967	2335337
White blood cell count decreased	267.90	27.31	128	5653	18080	2334224
Neutropenia	261.99	27.31	133	5648	21415	2330889
Drug ineffective	233.52	27.31	224	5557	101400	2250904
Asthenia	227.48	27.31	160	5621	46766	2305538
Cytogenetic analysis abnormal	226.18	27.31	38	5743	70	2352234
Leukaemia recurrent	224.88	27.31	43	5738	209	2352095
Abdominal pain	221.52	27.31	140	5641	34234	2318070
Bone marrow failure	220.74	27.31	80	5701	5606	2346698
Malaise	216.35	27.31	166	5615	55419	2296885
Chromosome analysis abnormal	215.83	27.31	34	5747	31	2352273
Platelet count decreased	196.08	27.31	99	5682	15714	2336590
Pneumonia	191.20	27.31	147	5634	49149	2303155
Swelling face	177.79	27.31	79	5702	9414	2342890
Blood creatinine increased	176.17	27.31	81	5700	10452	2341852
Metastases to liver	175.06	27.31	57	5724	2884	2349420
Ascites	173.99	27.31	67	5714	5553	2346751
Eyelid oedema	173.10	27.31	55	5726	2571	2349733
Pericardial effusion	172.89	27.31	61	5720	3948	2348356
Neoplasm progression	171.19	27.31	63	5718	4605	2347699
Generalised oedema	169.49	27.31	53	5728	2350	2349954
Leukopenia	169.24	27.31	78	5703	10118	2342186
Normal newborn	168.56	27.31	46	5735	1254	2351050
Abdominal pain upper	167.64	27.31	100	5681	22000	2330304
Headache	159.98	27.31	164	5617	80015	2272289
Face oedema	158.61	27.31	57	5724	3891	2348413
Acute lymphocytic leukaemia recurrent	155.20	27.31	31	5750	196	2352108
Myalgia	155.00	27.31	97	5684	23236	2329068
White blood cell count increased	152.37	27.31	65	5716	7013	2345291
Hepatotoxicity	150.21	27.31	53	5728	3428	2348876
Aspartate aminotransferase increased	147.65	27.31	76	5705	12536	2339768
Pruritus	145.87	27.31	119	5662	43221	2309083
Alanine aminotransferase increased	145.61	27.31	78	5703	13954	2338350
Decreased appetite	143.10	27.31	100	5681	28791	2323513
Gastric antral vascular ectasia	142.14	27.31	26	5755	94	2352210
Weight increased	138.69	27.31	89	5692	22248	2330056
Blister	135.29	27.31	59	5722	6712	2345592
Therapeutic response decreased	135.06	27.31	60	5721	7135	2345169
Weight decreased	128.48	27.31	93	5688	28278	2324026
Bone pain	125.26	27.31	61	5720	8935	2343369
Haematocrit decreased	124.83	27.31	49	5732	4269	2348035
General physical health deterioration	120.35	27.31	69	5712	14070	2338234
Jaundice	119.89	27.31	51	5730	5457	2346847
Blood alkaline phosphatase increased	117.78	27.31	53	5728	6492	2345812
Pain in extremity	116.85	27.31	104	5677	42436	2309868
Cough	115.68	27.31	93	5688	33024	2319280
Alopecia	115.56	27.31	79	5702	21922	2330382
Surgery	113.07	27.31	49	5732	5486	2346818
Blood lactate dehydrogenase increased	109.44	27.31	42	5739	3442	2348862
Maternal exposure during pregnancy	109.32	27.31	66	5715	14797	2337507
Sepsis	108.16	27.31	71	5710	18417	2333887
Red blood cell count decreased	108.00	27.31	44	5737	4222	2348082
Arthralgia	107.89	27.31	111	5670	54174	2298130
Platelet count increased	107.82	27.31	37	5744	2200	2350104
Splenomegaly	104.31	27.31	33	5748	1518	2350786
Right ventricular failure	103.37	27.31	36	5745	2237	2350067
Philadelphia chromosome positive	102.74	27.31	17	5764	27	2352277
Leukocytosis	101.31	27.31	40	5741	3536	2348768
Therapy non-responder	101.07	27.31	51	5730	8053	2344251
Dehydration	100.67	27.31	73	5708	22222	2330082
Abdominal distension	99.95	27.31	55	5726	10356	2341948
Breast cancer	99.05	27.31	53	5728	9442	2342862
Gastrointestinal haemorrhage	98.68	27.31	58	5723	12377	2339927
Swelling	98.58	27.31	64	5717	16286	2336018
Abortion spontaneous	97.05	27.31	59	5722	13386	2338918
Pain	95.91	27.31	111	5670	61746	2290558
Abdominal discomfort	94.76	27.31	64	5717	17392	2334912
Treatment failure	94.52	27.31	47	5734	7192	2345112
Respiratory failure	94.16	27.31	58	5723	13470	2338834
Graft versus host disease	92.79	27.31	27	5754	932	2351372
Dry skin	92.24	27.31	45	5736	6607	2345697
Chronic graft versus host disease	90.59	27.31	22	5759	371	2351933
Conjunctival haemorrhage	90.11	27.31	24	5757	594	2351710
Growth retardation	89.06	27.31	20	5761	235	2352069
Haematotoxicity	87.56	27.31	27	5754	1140	2351164
Blood bilirubin increased	85.83	27.31	40	5741	5305	2346999
Acute lymphocytic leukaemia	85.77	27.31	22	5759	468	2351836
Renal failure	85.65	27.31	60	5721	17289	2335015
Cardiac failure congestive	84.92	27.31	58	5723	16043	2336261
Recurrent cancer	83.57	27.31	20	5761	316	2351988
Eye haemorrhage	83.43	27.31	27	5754	1336	2350968
Pseudoporphyria	82.93	27.31	15	5766	50	2352254
Metastases to peritoneum	82.30	27.31	21	5760	437	2351867
Hepatitis	82.30	27.31	41	5740	6296	2346008
Exposure via body fluid	82.00	27.31	19	5762	259	2352045
Thrombocytosis	80.49	27.31	24	5757	903	2351401
Drug interaction	79.37	27.31	71	5710	29092	2323212
Febrile neutropenia	79.15	27.31	48	5733	10834	2341470
Neoplasm recurrence	78.90	27.31	20	5761	405	2351899
Ejection fraction decreased	78.17	27.31	31	5750	2770	2349534
Lacrimation increased	77.86	27.31	31	5750	2799	2349505
Erythema	75.98	27.31	65	5716	25094	2327210
Product use in unapproved indication	75.33	27.31	47	5734	11153	2341151
Gamma-glutamyltransferase increased	75.23	27.31	37	5744	5525	2346779
Chronic myeloid leukaemia transformation	74.22	27.31	13	5768	34	2352270
Gastrooesophageal reflux disease	73.65	27.31	43	5738	9052	2343252
Lung infiltration	73.62	27.31	28	5753	2236	2350068
Chest pain	73.60	27.31	67	5714	28070	2324234
Liver function test abnormal	73.05	27.31	40	5741	7450	2344854
Hepatic failure	71.49	27.31	36	5745	5653	2346651
Interstitial lung disease	71.48	27.31	40	5741	7772	2344532
Septic shock	69.70	27.31	38	5743	7016	2345288
Constipation	69.65	27.31	58	5723	21571	2330733
Renal impairment	69.51	27.31	43	5738	10049	2342255
Cardiotoxicity	69.45	27.31	23	5758	1224	2351080
Drug level increased	67.98	27.31	28	5753	2759	2349545
Caesarean section	66.94	27.31	31	5750	4050	2348254
Neutrophil count decreased	66.62	27.31	36	5745	6531	2345773
Gastrointestinal disorder	66.56	27.31	40	5741	8877	2343427
Visual impairment	65.91	27.31	44	5737	11711	2340593
Infection	65.76	27.31	52	5729	17977	2334327
Acute myeloid leukaemia	65.33	27.31	27	5754	2683	2349621
Skin exfoliation	65.11	27.31	34	5747	5756	2346548
Blood urea increased	64.20	27.31	29	5752	3576	2348728
Blood creatine phosphokinase increased	63.07	27.31	32	5749	5104	2347200
Disseminated intravascular coagulation	63.02	27.31	28	5753	3322	2348982
C-reactive protein increased	62.64	27.31	34	5747	6221	2346083
Mucosal inflammation	62.55	27.31	32	5749	5192	2347112
Cardiac failure	62.40	27.31	43	5738	12051	2340253
Acute kidney injury	62.13	27.31	61	5720	28061	2324243
Eye oedema	61.73	27.31	16	5765	355	2351949
Cerebrovascular accident	60.61	27.31	52	5729	20134	2332170
Transaminases increased	60.50	27.31	30	5751	4557	2347747
Joint swelling	60.24	27.31	48	5733	16771	2335533
Lung disorder	60.09	27.31	33	5748	6179	2346125
Myelodysplastic syndrome	60.00	27.31	25	5756	2535	2349769
Gait disturbance	59.55	27.31	54	5727	22491	2329813
Chills	59.18	27.31	46	5735	15506	2336798
Abortion induced	59.17	27.31	27	5754	3409	2348895
Liver disorder	59.10	27.31	33	5748	6381	2345923
Depression	58.41	27.31	59	5722	28073	2324231
Leukaemia	58.04	27.31	18	5763	774	2351530
Left ventricular dysfunction	57.76	27.31	20	5761	1220	2351084
Eosinophilia	56.43	27.31	25	5756	2945	2349359
Bone marrow transplant	56.04	27.31	13	5768	178	2352126
Pulmonary oedema	54.86	27.31	33	5748	7330	2344974
Hypoaesthesia	54.52	27.31	49	5732	20166	2332138
Computerised tomogram abnormal	54.07	27.31	15	5766	434	2351870
Cytogenetic abnormality	53.43	27.31	12	5769	141	2352163
Dyspepsia	53.15	27.31	36	5745	9808	2342496
Dizziness	53.14	27.31	81	5700	58584	2293720
Neuropathy peripheral	52.83	27.31	38	5743	11394	2340910
Atelectasis	52.23	27.31	21	5760	1944	2350360
Hepatic necrosis	52.07	27.31	18	5763	1092	2351212
Tumour excision	51.84	27.31	11	5770	97	2352207
Chronic myeloid leukaemia recurrent	51.82	27.31	9	5772	22	2352282
Hypersensitivity	51.77	27.31	51	5730	23542	2328762
Premature labour	50.82	27.31	21	5760	2085	2350219
Peripheral swelling	50.12	27.31	44	5737	17553	2334751
Acute graft versus host disease	49.73	27.31	15	5766	587	2351717
Papilloedema	49.44	27.31	16	5765	791	2351513
Flatulence	49.24	27.31	26	5755	4499	2347805
Back pain	49.23	27.31	57	5724	31602	2320702
Blood test abnormal	49.05	27.31	18	5763	1300	2351004
Ocular hyperaemia	49.00	27.31	25	5756	4031	2348273
Respiratory distress	48.92	27.31	27	5754	5102	2347202
Exposure via father	48.88	27.31	12	5769	212	2352092
Multiple organ dysfunction syndrome	48.69	27.31	31	5750	7610	2344694
Palpitations	48.59	27.31	42	5739	16414	2335890
Blast cells present	48.44	27.31	10	5771	76	2352228
Premature baby	48.41	27.31	23	5758	3181	2349123
Musculoskeletal pain	47.76	27.31	35	5746	10795	2341509
Hepatomegaly	46.93	27.31	19	5762	1790	2350514
Hypoxia	46.63	27.31	28	5753	6199	2346105
Dyspnoea exertional	46.17	27.31	27	5754	5693	2346611
Hypokalaemia	46.01	27.31	34	5747	10620	2341684
Pulse waveform abnormal	45.79	27.31	7	5774	4	2352300
Ankle brachial index decreased	45.79	27.31	7	5774	4	2352300
Pneumatosis intestinalis	45.79	27.31	13	5768	410	2351894
Rash erythematous	45.08	27.31	27	5754	5949	2346355
Hepatic function abnormal	44.60	27.31	27	5754	6065	2346239
Insomnia	44.46	27.31	49	5732	25738	2326566
Toxicity to various agents	44.40	27.31	55	5726	32699	2319605
Metastases to lung	44.28	27.31	18	5763	1713	2350591
Chloroma	44.25	27.31	9	5772	63	2352241
Neoplasm	43.98	27.31	16	5765	1127	2351177
Myelofibrosis	43.98	27.31	12	5769	326	2351978
Condition aggravated	43.83	27.31	54	5727	31925	2320379
Carotid intima-media thickness increased	43.62	27.31	7	5774	8	2352296
Myocardial infarction	43.38	27.31	42	5739	18971	2333333
Colitis	43.06	27.31	25	5756	5201	2347103
Subdural haematoma	42.97	27.31	19	5762	2227	2350077
Blindness	42.84	27.31	22	5759	3596	2348708
Stem cell transplant	42.52	27.31	12	5769	370	2351934
Bronchopulmonary aspergillosis	42.19	27.31	15	5766	989	2351315
Morphoea	42.15	27.31	9	5772	82	2352222
Aspiration pleural cavity	42.08	27.31	10	5771	153	2352151
Tumour necrosis	40.66	27.31	10	5771	178	2352126
Cardiac output decreased	40.60	27.31	10	5771	179	2352125
Skin fragility	40.45	27.31	9	5772	101	2352203
Feeling abnormal	39.25	27.31	44	5737	23537	2328767
Eye pain	39.25	27.31	23	5758	4868	2347436
Urine odour abnormal	38.87	27.31	13	5768	713	2351591
Tumour haemorrhage	38.86	27.31	11	5770	343	2351961
Blood blister	38.68	27.31	11	5770	349	2351955
Hypothyroidism	38.53	27.31	22	5759	4435	2347869
Lymphadenopathy	38.51	27.31	24	5757	5674	2346630
Bronchitis	38.46	27.31	34	5747	13680	2338624
Vision blurred	38.44	27.31	35	5746	14633	2337671
Hypoacusis	38.17	27.31	20	5761	3405	2348899
Glaucoma	37.76	27.31	17	5764	2078	2350226
Tumour lysis syndrome	37.50	27.31	14	5767	1061	2351243
Skin disorder	37.08	27.31	20	5761	3611	2348693
Blood albumin decreased	36.98	27.31	16	5765	1779	2350525
Acute hepatic failure	36.98	27.31	18	5763	2624	2349680
Dysphagia	36.41	27.31	32	5749	12773	2339531
Atrial fibrillation	36.36	27.31	33	5748	13735	2338569
Photophobia	36.32	27.31	17	5764	2272	2350032
Blood uric acid increased	36.04	27.31	12	5769	649	2351655
Gene mutation	35.94	27.31	9	5772	173	2352131
Renal disorder	35.73	27.31	21	5760	4467	2347837
Exposure via partner	35.69	27.31	8	5773	93	2352211
Gastric cancer	35.62	27.31	12	5769	673	2351631
Blood glucose increased	35.52	27.31	31	5750	12259	2340045
Aplasia	35.40	27.31	11	5770	476	2351828
Hepatic enzyme increased	35.13	27.31	28	5753	9774	2342530
Cytopenia	34.68	27.31	13	5768	996	2351308
Mitral valve incompetence	34.57	27.31	17	5764	2533	2349771
Fall	34.37	27.31	59	5722	47040	2305264
Dialysis	34.09	27.31	16	5765	2151	2350153
Parosmia	33.72	27.31	12	5769	793	2351511
Uterine cancer	33.45	27.31	12	5769	812	2351492
Product substitution issue	33.37	27.31	21	5760	5048	2347256
Peripheral arterial occlusive disease	33.34	27.31	11	5770	578	2351726
Gastrectomy	33.32	27.31	8	5773	128	2352176
Dermatitis bullous	32.94	27.31	14	5767	1490	2350814
Thrombosis	32.51	27.31	26	5755	9118	2343186
Coagulopathy	32.46	27.31	17	5764	2892	2349412
Contusion	32.46	27.31	30	5751	12780	2339524
Muscular weakness	32.27	27.31	32	5749	14865	2337439
Haemorrhage	32.21	27.31	28	5753	11011	2341293
Dysgeusia	32.11	27.31	25	5756	8434	2343870
Lichen planus	31.89	27.31	10	5771	446	2351858
Cardiac disorder	31.59	27.31	24	5757	7809	2344495
Chordoma	31.50	27.31	5	5776	5	2352299
Paraesthesia	31.38	27.31	38	5743	22050	2330254
Drug eruption	30.64	27.31	17	5764	3242	2349062
Blast cell crisis	30.44	27.31	6	5775	35	2352269
Gastric haemorrhage	30.36	27.31	12	5769	1061	2351243
Memory impairment	30.32	27.31	29	5752	12894	2339410
Haematochezia	30.09	27.31	20	5761	5275	2347029
Visual acuity reduced	30.08	27.31	20	5761	5278	2347026
Blood potassium decreased	30.06	27.31	20	5761	5285	2347019
Lichenoid keratosis	29.93	27.31	9	5772	348	2351956
Skin lesion	29.87	27.31	18	5763	4007	2348297
Disease recurrence	29.73	27.31	17	5764	3434	2348870
Tachycardia	29.69	27.31	32	5749	16377	2335927
Urine output decreased	29.54	27.31	13	5768	1506	2350798
Somnolence	29.52	27.31	38	5743	23447	2328857
Trisomy 8	29.48	27.31	5	5776	10	2352294
Electrocardiogram QT prolonged	29.45	27.31	23	5758	7791	2344513
Rash maculo-papular	28.96	27.31	18	5763	4234	2348070
Blood sodium decreased	28.68	27.31	16	5765	3084	2349220
Anxiety	28.61	27.31	42	5739	29317	2322987
Blood iron decreased	28.45	27.31	12	5769	1253	2351051
Feeling cold	28.44	27.31	16	5765	3134	2349170
Diabetes mellitus	28.12	27.31	22	5759	7473	2344831
Ileus	28.02	27.31	14	5767	2158	2350146
Slit-lamp tests abnormal	27.97	27.31	4	5777	0	2352304
Odynophagia	27.96	27.31	11	5770	961	2351343
Hepatic enzyme abnormal	27.91	27.31	10	5771	674	2351630
Hypertension	27.91	27.31	40	5741	27321	2324983
Graft versus host disease in skin	27.71	27.31	8	5773	268	2352036
Polyneuropathy	27.68	27.31	13	5768	1750	2350554
Swollen tongue	27.54	27.31	19	5762	5324	2346980
Squamous cell carcinoma	27.42	27.31	12	5769	1371	2350933
Bone marrow oedema	27.41	27.31	7	5774	146	2352158

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	1242.39	26.96	716	5512	86727	1653826
Neoplasm malignant	893.28	26.96	249	5979	4090	1736463
Chronic myeloid leukaemia	847.17	26.96	169	6059	529	1740024
Drug resistance	826.07	26.96	220	6008	3010	1737543
Malignant neoplasm progression	812.69	26.96	308	5920	13850	1726703
Blast crisis in myelogenous leukaemia	681.55	26.96	118	6110	108	1740445
Gastrointestinal stromal tumour	671.82	26.96	127	6101	269	1740284
Pleural effusion	527.31	26.96	211	6017	10899	1729654
Nausea	485.68	26.96	328	5900	50868	1689685
Diarrhoea	398.95	26.96	297	5931	53555	1686998
Pyrexia	377.51	26.96	271	5957	46129	1694424
Haemoglobin decreased	376.67	26.96	190	6038	16924	1723629
Anaemia	375.59	26.96	228	6000	29229	1711324
Second primary malignancy	327.19	26.96	84	6144	975	1739578
Muscle spasms	315.34	26.96	149	6079	11472	1729081
Dyspnoea	312.83	26.96	254	5974	51805	1688748
Fatigue	307.68	26.96	249	5979	50532	1690021
Vomiting	300.06	26.96	219	6009	38096	1702457
Disease progression	289.64	26.96	160	6068	17103	1723450
Oedema peripheral	285.47	26.96	153	6075	15397	1725156
Thrombocytopenia	279.34	26.96	168	6060	21081	1719472
Neoplasm progression	276.01	26.96	95	6133	3172	1737381
Rash	269.00	26.96	206	6022	38487	1702066
Metastases to liver	268.11	26.96	85	6143	2182	1738371
Abdominal pain	259.62	26.96	161	6067	21329	1719224
Drug intolerance	258.97	26.96	107	6121	5955	1734598
Platelet count decreased	257.63	26.96	146	6082	16377	1724176
Drug ineffective	254.62	26.96	247	5981	63554	1676999
Leukaemia recurrent	254.41	26.96	54	6174	245	1740308
Pancytopenia	246.19	26.96	125	6103	11232	1729321
Ascites	243.34	26.96	100	6128	5486	1735067
Blood creatinine increased	219.34	26.96	124	6104	13822	1726731
Therapeutic response decreased	217.79	26.96	92	6136	5408	1735145
Chromosome analysis abnormal	210.94	26.96	36	6192	27	1740526
Periorbital oedema	201.37	26.96	53	6175	681	1739872
Asthenia	196.59	26.96	164	6064	34506	1706047
White blood cell count increased	195.72	26.96	93	6135	7219	1733334
Prostate cancer	195.25	26.96	81	6147	4545	1736008
Oedema	190.96	26.96	90	6138	6858	1733695
Fluid retention	189.28	26.96	75	6153	3734	1736819
Pneumonia	185.87	26.96	180	6048	46002	1694551
White blood cell count decreased	169.91	26.96	103	6125	13046	1727507
Splenomegaly	168.72	26.96	59	6169	2061	1738492
Gene mutation identification test positive	168.46	26.96	31	6197	52	1740501
Neutropenia	164.48	26.96	114	6114	18146	1722407
Treatment failure	155.65	26.96	68	6160	4333	1736220
Arthralgia	154.01	26.96	121	6107	23323	1717230
Bone marrow failure	150.99	26.96	70	6158	5130	1735423
Myalgia	146.24	26.96	100	6128	15558	1724995
Surgery	144.38	26.96	57	6171	2806	1737747
Acute lymphocytic leukaemia recurrent	144.13	26.96	34	6194	268	1740285
Malaise	143.30	26.96	128	6100	29437	1711116
Neoplasm recurrence	143.11	26.96	36	6192	381	1740172
Decreased appetite	139.34	26.96	115	6113	23756	1716797
Cytogenetic analysis abnormal	138.00	26.96	26	6202	53	1740500
Sepsis	135.58	26.96	104	6124	19334	1721219
Haematocrit decreased	131.80	26.96	60	6168	4213	1736340
Pain in extremity	129.18	26.96	99	6129	18373	1722180
Bone pain	128.87	26.96	55	6173	3307	1737246
Cardiac failure	123.61	26.96	83	6145	12519	1728034
Pain	116.55	26.96	109	6119	26548	1714005
Face oedema	115.99	26.96	46	6182	2290	1738263
General physical health deterioration	115.88	26.96	81	6147	13037	1727516
Graft versus host disease	115.07	26.96	41	6187	1512	1739041
Philadelphia chromosome positive	115.00	26.96	20	6208	19	1740534
Product use in unapproved indication	114.43	26.96	71	6157	9351	1731202
Red blood cell count decreased	114.43	26.96	52	6176	3634	1736919
Gene mutation	113.65	26.96	25	6203	138	1740415
Therapy non-responder	112.80	26.96	61	6167	6205	1734348
Pericardial effusion	112.15	26.96	50	6178	3340	1737213
Respiratory failure	108.56	26.96	81	6147	14424	1726129
Blood lactate dehydrogenase increased	108.29	26.96	50	6178	3625	1736928
Pruritus	107.38	26.96	98	6130	23124	1717429
Weight decreased	105.16	26.96	96	6132	22657	1717896
Acquired gene mutation	103.85	26.96	24	6204	171	1740382
Ejection fraction decreased	103.81	26.96	42	6186	2203	1738350
Blast cell count increased	103.60	26.96	24	6204	173	1740380
Blood alkaline phosphatase increased	103.16	26.96	54	6174	5141	1735412
Renal failure	101.47	26.96	89	6139	19928	1720625
Chronic myeloid leukaemia recurrent	97.14	26.96	18	6210	32	1740521
Chronic myeloid leukaemia transformation	92.99	26.96	18	6210	45	1740508
Abdominal distension	92.27	26.96	54	6174	6390	1734163
Abdominal discomfort	91.85	26.96	61	6167	9020	1731533
Cough	88.66	26.96	81	6147	19116	1721437
Abdominal pain upper	88.05	26.96	64	6164	10937	1729616
Chronic graft versus host disease	87.46	26.96	26	6202	532	1740021
Eyelid oedema	87.29	26.96	32	6196	1281	1739272
Blast cell crisis	86.32	26.96	17	6211	48	1740505
Recurrent cancer	86.25	26.96	22	6206	247	1740306
Alanine aminotransferase increased	86.15	26.96	66	6162	12212	1728341
Myelofibrosis	86.14	26.96	24	6204	386	1740167
Multiple organ dysfunction syndrome	86.10	26.96	59	6169	9183	1731370
Interstitial lung disease	85.87	26.96	60	6168	9636	1730917
Metastases to peritoneum	85.71	26.96	23	6205	319	1740234
Blood urea increased	85.14	26.96	46	6182	4665	1735888
Cytogenetic abnormality	84.35	26.96	21	6207	212	1740341
Aspartate aminotransferase increased	82.52	26.96	61	6167	10695	1729858
Generalised oedema	81.63	26.96	33	6195	1726	1738827
Colon cancer	79.78	26.96	33	6195	1831	1738722
Leukocytosis	79.60	26.96	40	6188	3493	1737060
Stem cell transplant	78.62	26.96	23	6205	444	1740109
Renal impairment	77.32	26.96	62	6166	12252	1728301
Cardiomyopathy	76.58	26.96	36	6192	2716	1737837
Acute myeloid leukaemia	76.15	26.96	37	6191	3004	1737549
Blood bilirubin increased	75.86	26.96	47	6181	6163	1734390
Lymphadenopathy	73.86	26.96	40	6188	4074	1736479
Gastric antral vascular ectasia	71.18	26.96	15	6213	65	1740488
Chest pain	71.15	26.96	73	6155	19841	1720712
Headache	70.91	26.96	95	6133	34281	1706272
Gastric cancer	70.41	26.96	26	6202	1062	1739491
Blindness	69.95	26.96	34	6194	2762	1737791
Infection	68.74	26.96	58	6170	12302	1728251
Eye swelling	68.48	26.96	30	6198	1919	1738634
Dehydration	67.22	26.96	67	6161	17591	1722962
Bone marrow necrosis	66.37	26.96	14	6214	61	1740492
Dyspnoea exertional	65.22	26.96	37	6191	4124	1736429
Blood creatine phosphokinase increased	65.17	26.96	49	6179	8807	1731746
Skin lesion	65.05	26.96	33	6195	2939	1737614
Cardiac failure congestive	63.84	26.96	61	6167	15209	1725344
Swelling face	62.66	26.96	37	6191	4446	1736107
Weight increased	62.54	26.96	53	6175	11304	1729249
Swelling	61.23	26.96	43	6185	6953	1733600
Platelet count increased	60.37	26.96	26	6202	1595	1738958
Gastrointestinal haemorrhage	59.65	26.96	57	6171	14210	1726343
Gait disturbance	59.48	26.96	54	6174	12616	1727937
Chloroma	56.56	26.96	13	6215	90	1740463
Dizziness	56.13	26.96	85	6143	34276	1706277
Bone marrow transplant	55.56	26.96	15	6213	213	1740340
Multiple-drug resistance	55.42	26.96	16	6212	294	1740259
Muscular weakness	54.73	26.96	47	6181	10202	1730351
Skin exfoliation	54.55	26.96	34	6194	4501	1736052
Septic shock	53.38	26.96	42	6186	8067	1732486
Tumour haemorrhage	53.37	26.96	18	6210	561	1739992
Pseudoporphyria	53.27	26.96	12	6216	75	1740478
Atrial fibrillation	53.23	26.96	55	6173	15056	1725497
Lung disorder	53.20	26.96	35	6193	5084	1735469
Palpitations	53.02	26.96	39	6189	6775	1733778
Drug interaction	51.18	26.96	73	6155	27885	1712668
Exposure via father	51.03	26.96	12	6216	93	1740460
Dysphagia	51.01	26.96	45	6183	10123	1730430
Hypoxia	50.66	26.96	36	6192	5927	1734626
Back pain	50.63	26.96	56	6172	16557	1723996
Erythema	50.62	26.96	52	6176	14136	1726417
Blast cells present	50.11	26.96	11	6217	60	1740493
Hepatotoxicity	49.88	26.96	28	6200	3056	1737497
Hepatomegaly	49.84	26.96	23	6205	1662	1738891
Myocardial infarction	49.81	26.96	71	6157	27103	1713450
Hypoalbuminaemia	49.75	26.96	22	6206	1438	1739115
Subdural haematoma	49.53	26.96	29	6199	3428	1737125
Cerebral haemorrhage	49.00	26.96	36	6192	6241	1734312
Tumour lysis syndrome	48.99	26.96	23	6205	1728	1738825
Acute respiratory distress syndrome	48.81	26.96	29	6199	3522	1737031
Chordoma	48.78	26.96	8	6220	3	1740550
C-reactive protein increased	48.78	26.96	35	6193	5850	1734703
Peripheral swelling	47.60	26.96	39	6189	7932	1732621
Desmoid tumour	47.54	26.96	9	6219	19	1740534
Pulmonary oedema	47.46	26.96	36	6192	6550	1734003
Eosinophil count increased	47.38	26.96	21	6207	1380	1739173
Hepatitis	46.98	26.96	32	6196	4923	1735630
Lung neoplasm malignant	46.42	26.96	27	6201	3152	1737401
Hepatic failure	46.41	26.96	34	6194	5869	1734684
Gastrectomy	46.36	26.96	11	6217	89	1740464
Haemorrhage	46.33	26.96	42	6186	9787	1730766
Pneumonitis	46.20	26.96	29	6199	3886	1736667
Chronic kidney disease	46.04	26.96	30	6198	4287	1736266
Condition aggravated	45.92	26.96	60	6168	21090	1719463
Jaundice	45.60	26.96	34	6194	6028	1734525
Cardiomegaly	45.55	26.96	24	6204	2310	1738243
Metastases to lung	45.55	26.96	21	6207	1514	1739039
Acute kidney injury	45.50	26.96	78	6150	34866	1705687
Tumour excision	45.03	26.96	10	6218	58	1740495
Hepatic lesion	44.18	26.96	15	6213	477	1740076
Visual acuity reduced	43.88	26.96	28	6200	3860	1736693
Myocardial ischaemia	43.68	26.96	26	6202	3167	1737386
Leukopenia	43.47	26.96	38	6190	8442	1732111
Melaena	43.21	26.96	31	6197	5179	1735374
Growth retardation	43.17	26.96	15	6213	512	1740041
Myelodysplastic syndrome	42.97	26.96	26	6202	3263	1737290
Metastases to lymph nodes	42.78	26.96	17	6211	849	1739704
Bone marrow oedema	42.60	26.96	11	6217	130	1740423
Tumour necrosis	42.27	26.96	12	6216	207	1740346
Haematotoxicity	41.12	26.96	17	6211	941	1739612
Disseminated intravascular coagulation	40.72	26.96	26	6202	3588	1736965
Visual impairment	40.47	26.96	32	6196	6186	1734367
Depression	40.45	26.96	50	6178	16619	1723934
Marrow hyperplasia	40.00	26.96	11	6217	168	1740385
Dyspepsia	39.83	26.96	29	6199	4956	1735597
Metastasis	39.83	26.96	16	6212	822	1739731
Constipation	39.67	26.96	47	6181	14953	1725600
Scleroderma	39.40	26.96	12	6216	267	1740286
Cerebrovascular accident	39.26	26.96	51	6177	17815	1722738
Gamma-glutamyltransferase increased	39.25	26.96	29	6199	5069	1735484
Complications of transplant surgery	39.22	26.96	10	6218	112	1740441
Transaminases increased	38.81	26.96	26	6202	3891	1736662
Gastrointestinal disorder	38.80	26.96	28	6200	4720	1735833
Lung infiltration	38.76	26.96	21	6207	2138	1738415
Post embolisation syndrome	38.71	26.96	7	6221	10	1740543
Myositis	38.61	26.96	19	6209	1584	1738969
Rash erythematous	38.52	26.96	26	6202	3939	1736614
Concomitant disease aggravated	37.96	26.96	15	6213	738	1739815
Rales	37.86	26.96	16	6212	936	1739617
Blood blister	37.67	26.96	12	6216	311	1740242
Gastrooesophageal reflux disease	37.05	26.96	27	6201	4620	1735933
Neutrophil count decreased	36.82	26.96	30	6198	6051	1734502
Confusional state	36.63	26.96	54	6174	21224	1719329
Hepatic enzyme increased	36.63	26.96	31	6197	6590	1733963
Bone marrow disorder	36.56	26.96	12	6216	343	1740210
Gastritis	36.55	26.96	23	6205	3094	1737459
Cardiac disorder	36.50	26.96	33	6195	7658	1732895
Ileus	36.31	26.96	21	6207	2425	1738128
Chest expansion decreased	36.30	26.96	7	6221	17	1740536
Acute graft versus host disease	36.25	26.96	15	6213	832	1739721
Tuberculosis	35.88	26.96	19	6209	1847	1738706
Vision blurred	35.83	26.96	34	6194	8389	1732164
Disease recurrence	35.25	26.96	21	6207	2561	1737992
Lung adenocarcinoma	35.10	26.96	14	6214	706	1739847
Hyperbilirubinaemia	34.92	26.96	20	6208	2267	1738286
Hepatitis B	34.90	26.96	17	6211	1386	1739167
Cytopenia	34.80	26.96	15	6213	921	1739632
Pneumothorax	34.30	26.96	21	6207	2691	1737862
Bladder cancer	34.15	26.96	19	6209	2037	1738516
Metastases to heart	34.02	26.96	8	6220	62	1740491
Drug level increased	33.84	26.96	21	6207	2756	1737797
Leukaemia	33.70	26.96	14	6214	784	1739769
Amylase increased	33.66	26.96	16	6212	1236	1739317
Hypokalaemia	33.54	26.96	29	6199	6345	1734208
Fall	33.12	26.96	59	6169	27155	1713398
Haematuria	33.08	26.96	31	6197	7529	1733024
Product substitution issue	33.00	26.96	22	6206	3264	1737289
Clonal evolution	32.62	26.96	6	6222	10	1740543
Protein total decreased	32.54	26.96	13	6215	658	1739895
Pancreatitis	32.47	26.96	30	6198	7157	1733396
Osteomyelitis	32.21	26.96	19	6209	2276	1738277
Conjunctival haemorrhage	32.08	26.96	12	6216	508	1740045
Pigmentation disorder	32.03	26.96	12	6216	510	1740043
Left ventricular failure	32.01	26.96	13	6215	687	1739866
Joint swelling	31.61	26.96	28	6200	6325	1734228
Eosinophilia	31.59	26.96	22	6206	3505	1737048
Hypertension	31.53	26.96	48	6180	19400	1721153
Diabetes mellitus	31.52	26.96	29	6199	6879	1733674
Cholestasis	30.83	26.96	22	6206	3643	1736910
Graft versus host disease in skin	30.58	26.96	11	6217	416	1740137
Blood uric acid increased	30.55	26.96	14	6214	995	1739558
Chills	29.87	26.96	36	6192	11651	1728902
Biopsy bone marrow abnormal	29.80	26.96	8	6220	111	1740442
Thrombocytosis	29.79	26.96	12	6216	621	1739932
Lipase increased	29.72	26.96	16	6212	1608	1738945
Febrile neutropenia	29.70	26.96	35	6193	11065	1729488
Mitral valve incompetence	29.70	26.96	17	6211	1925	1738628
Neoplasm	29.64	26.96	13	6215	833	1739720
Hyperkeratosis	29.59	26.96	12	6216	632	1739921
Central nervous system leukaemia	29.57	26.96	7	6221	56	1740497
Blood albumin decreased	29.50	26.96	16	6212	1632	1738921
Chest X-ray abnormal	29.42	26.96	12	6216	641	1739912
Haemoptysis	29.40	26.96	24	6204	4852	1735701
Hepatic function abnormal	29.03	26.96	28	6200	7046	1733507
Productive cough	28.93	26.96	21	6207	3570	1736983
Metastases to bone	28.70	26.96	16	6212	1722	1738831
Dysgeusia	28.66	26.96	24	6204	5025	1735528
Aspiration pleural cavity	28.63	26.96	8	6220	130	1740423
Venoocclusive liver disease	28.42	26.96	13	6215	920	1739633
Pleural fibrosis	28.37	26.96	9	6219	230	1740323
Liver disorder	28.36	26.96	25	6203	5611	1734942
Concomitant disease progression	28.23	26.96	11	6217	521	1740032
Chest discomfort	28.19	26.96	28	6200	7303	1733250
Renal cell carcinoma	27.99	26.96	15	6213	1493	1739060
Acute lymphocytic leukaemia	27.68	26.96	11	6217	549	1740004
Intra-abdominal haemorrhage	27.63	26.96	10	6218	385	1740168
Eating disorder	27.57	26.96	14	6214	1248	1739305
Bronchopulmonary aspergillosis	27.46	26.96	15	6213	1551	1739002
Inflammation	27.40	26.96	20	6208	3430	1737123
Haematemesis	27.35	26.96	22	6206	4355	1736198
Nephrectomy	27.31	26.96	8	6220	155	1740398
Acute myeloid leukaemia recurrent	27.29	26.96	9	6219	261	1740292
Optic neuritis	27.28	26.96	12	6216	774	1739779
Dilatation ventricular	27.25	26.96	11	6217	572	1739981
Haematochezia	27.08	26.96	23	6205	4909	1735644

Pharmacologic Action:

Source	Code	Description
ATC	L01XE01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS 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	antineoplastic agent

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)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 100MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or efficacy reasons	GLEEVEC	NOVARTIS	N021335	May 10, 2001	DISCN	CAPSULE	ORAL	6958335	Dec. 19, 2021	GLEEVEC IS ALSO INDICATED FOR THE TREATMENT OF PATIENTS WITH KIT (CD117) POSITIVE UNRESECTABLE AND/OR METASTATIC MALIGNANT GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 50MG BASE Federal Register determination that product was not discontinued or withdrawn for safety or efficacy reasons	GLEEVEC	NOVARTIS	N021335	May 10, 2001	DISCN	CAPSULE	ORAL	6958335	Dec. 19, 2021	GLEEVEC IS ALSO INDICATED FOR THE TREATMENT OF PATIENTS WITH KIT (CD117) POSITIVE UNRESECTABLE AND/OR METASTATIC MALIGNANT GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 100MG BASE	GLEEVEC	NOVARTIS	N021588	April 18, 2003	RX	TABLET	ORAL	6958335	Dec. 19, 2021	GLEEVEC IS ALSO INDICATED FOR THE TREATMENT OF PATIENTS WITH KIT (CD117) POSITIVE UNRESECTABLE AND/OR METASTATIC MALIGNANT GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 100MG BASE	GLEEVEC	NOVARTIS	N021588	April 18, 2003	RX	TABLET	ORAL	6958335	Dec. 19, 2021	TREATMENT OF GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 400MG BASE	GLEEVEC	NOVARTIS	N021588	April 18, 2003	RX	TABLET	ORAL	6958335	Dec. 19, 2021	GLEEVEC IS ALSO INDICATED FOR THE TREATMENT OF PATIENTS WITH KIT (CD117) POSITIVE UNRESECTABLE AND/OR METASTATIC MALIGNANT GASTROINTESTINAL STROMAL TUMORS (GIST)
EQ 400MG BASE	GLEEVEC	NOVARTIS	N021588	April 18, 2003	RX	TABLET	ORAL	6958335	Dec. 19, 2021	TREATMENT OF GASTROINTESTINAL STROMAL TUMORS (GIST)

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 100MG BASE	GLEEVEC	NOVARTIS	N021588	April 18, 2003	RX	TABLET	ORAL	Jan. 25, 2020	TREATMENT OF PEDIATRIC PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY, APPROVED UNDER NDA #21588/S-037
EQ 400MG BASE	GLEEVEC	NOVARTIS	N021588	April 18, 2003	RX	TABLET	ORAL	Jan. 25, 2020	TREATMENT OF PEDIATRIC PATIENTS WITH NEWLY DIAGNOSED PHILADELPHIA CHROMOSOME-POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA (PH+ ALL) IN COMBINATION WITH CHEMOTHERAPY, APPROVED UNDER NDA #21588/S-037

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	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
D000068877	MESH_DESCRIPTOR_UI
4021257	VUID
N0000148698	NUI
C0935989	UMLSCUI
D01441	KEGG_DRUG
391634008	SNOMEDCT_US
d04758	MMSL
282388	RXNORM
4021257	VANDF
414460008	SNOMEDCT_US
009151	NDDF
8A1O1M485B	UNII
220127-57-1	SECONDARY_CAS_RN
8031	INN_ID
CHEMBL941	ChEMBL_ID
DB00619	DRUGBANK_ID
CHEMBL1642	ChEMBL_ID
CHEBI:45783	CHEBI
5291	PUBCHEM_CID
5687	IUPHAR_LIGAND_ID

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	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0249	TABLET, FILM COATED	400 mg	ORAL	ANDA	18 sections
Gleevec	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0401	TABLET	100 mg	ORAL	NDA	17 sections
Gleevec	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0649	TABLET	400 mg	ORAL	NDA	17 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7629	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0093-7630	TABLET, FILM COATED	400 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-2245	TABLET, FILM COATED	100 mg	ORAL	ANDA	17 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0378-2246	TABLET, FILM COATED	400 mg	ORAL	ANDA	17 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6621	TABLET, FILM COATED	400 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6901	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
imatinib mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	16714-704	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
imatinib mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	16714-705	TABLET, FILM COATED	400 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	42292-043	TABLET, FILM COATED	100 mg	ORAL	ANDA	17 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	42292-044	TABLET, FILM COATED	400 mg	ORAL	ANDA	17 sections
Imatinib	HUMAN PRESCRIPTION DRUG LABEL	1	43598-344	TABLET	100 mg	ORAL	ANDA	18 sections
Imatinib	HUMAN PRESCRIPTION DRUG LABEL	1	43598-345	TABLET	400 mg	ORAL	ANDA	18 sections
imatinib mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	47335-472	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
imatinib mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	47335-475	TABLET, FILM COATED	400 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	50268-426	TABLET, FILM COATED	100 mg	ORAL	ANDA	19 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	50268-427	TABLET, FILM COATED	400 mg	ORAL	ANDA	19 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	51407-269	TABLET, FILM COATED	100 mg	ORAL	ANDA	17 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	51407-270	TABLET, FILM COATED	400 mg	ORAL	ANDA	17 sections
IMATINIB MESYLATE	HUMAN PRESCRIPTION DRUG LABEL	1	51991-376	TABLET, COATED	100 mg	ORAL	ANDA	18 sections
IMATINIB MESYLATE	HUMAN PRESCRIPTION DRUG LABEL	1	51991-377	TABLET, COATED	400 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	59923-723	TABLET, COATED	100 mg	ORAL	ANDA	17 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	59923-724	TABLET, COATED	400 mg	ORAL	ANDA	17 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60429-925	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60429-926	TABLET, FILM COATED	400 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60505-2900	TABLET, FILM COATED	100 mg	ORAL	ANDA	18 sections
Imatinib Mesylate	HUMAN PRESCRIPTION DRUG LABEL	1	60505-2901	TABLET, FILM COATED	400 mg	ORAL	ANDA	18 sections