All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

axitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	4225	319460-85-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: axitinib inlyta AG 013736 AG-013736	A benzamide and indazole derivative that acts as a TYROSINE KINASE inhibitor of the VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR. It is used in the treatment of advanced RENAL CELL CARCINOMA. Molecular weight: 386.47 Formula: C22H18N4OS CLOGP: 3.19 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 70.67 ALOGS: -5.85 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Hosey CM, Chan R, Benet LZ
CL (Clearance)	5 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.00 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4.30 hours	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ
BA (Bioavailability)	58 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	AAK1,ABL1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,BTK,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK2,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,DDR1,DYRK1A,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,ERBB4,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK1,GRK2,GRK3,GSK3A,GSK3B,IGF1R,IKBKB,INSR,IRAK1,IRAK3,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK3,MAPK7,MAPK8,MAPK9,MAPKAPK2,MARK1,MARK2,MARK4,MELK,MET,MINK1,MST1R,MTOR,NTRK1,NTRK2,NUAK1,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKAA1,PRKAA2,PRKCD,PRKCZ,PRKDC,RIPK3,ROCK1,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK10,STK17A,STK33,SYK,TEK,TGFBR1,TNIK,TTK,TYRO3,UHMK1,ULK1,ULK2,YES1,ZAP70	137
kinase-selectivity-class	AAK1,ABL2,ACVR1B,ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2A,CAMK2B,CAMK2D,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK7,CDK9,CHEK1,CLK2,CLK4,CSF1R,CSK,DDR1,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,EIF2AK3,EPHA2,EPHB3,EPHB4,ERBB2,FGFR1,FGFR4,FLT1,FLT3,FLT4,FYN,GAK,GRK2,GSK3A,GSK3B,HASPIN,INSR,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K3,MAP2K4,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K3,MAP4K4,MAP4K5,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,MST1R,NTRK1,NTRK3,NUAK1,PAK4,PDGFRB,PDK1,PDPK1,PIK3CA,PIM3,PLK4,PRKAA1,PRKAA2,PRKCD,PRKCZ,PTK2,RET,RIPK1,RIPK3,ROCK1,ROCK2,SGK1,SIK2,SIK3,SRC,STK10,STK16,STK17A,STK33,STK4,SYK,TEK,TGFBR1,TNIK,TNK1,TTK,TYRO3,ULK1,ULK2,YES1,ZAP70	134
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
Jan. 27, 2012	FDA	PFIZER

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
Neoplasm progression	749.10	22.74	256	10363	44230	90573598
Diarrhoea	474.31	22.74	562	10057	938628	89679200
Death	397.96	22.74	367	10252	456184	90161644
Disease progression	309.74	22.74	205	10414	156410	90461418
Hypertension	276.62	22.74	302	10317	457230	90160598
Palmar-plantar erythrodysaesthesia syndrome	262.60	22.74	105	10514	27918	90589910
Dysphonia	253.72	22.74	131	10488	62953	90554875
Blood pressure increased	209.65	22.74	178	10441	197039	90420789
Fatigue	206.87	22.74	430	10189	1153593	89464235
Decreased appetite	197.21	22.74	231	10388	376309	90241519
Hypothyroidism	151.63	22.74	88	10531	53039	90564789
Stomatitis	136.06	22.74	164	10455	274534	90343294
Oral pain	117.42	22.74	63	10556	32620	90585208
Nausea	89.06	22.74	308	10311	1110008	89507820
Off label use	83.39	22.74	300	10319	1101952	89515876
Drug ineffective	75.86	22.74	34	10585	1384264	89233564
Weight decreased	70.04	22.74	144	10475	379766	90238062
Dehydration	66.57	22.74	97	10522	194350	90423478
Malignant neoplasm progression	63.15	22.74	70	10549	106800	90511028
Posterior reversible encephalopathy syndrome	58.43	22.74	35	10584	22304	90595524
Constipation	51.27	22.74	106	10513	280289	90337539
Proteinuria	49.55	22.74	32	10587	23259	90594569
Thyroid disorder	49.48	22.74	29	10590	17756	90600072
Asthenia	48.63	22.74	155	10464	533596	90084232
Immune-mediated hepatic disorder	40.85	22.74	13	10606	1779	90616049
Second primary malignancy	40.06	22.74	21	10598	10357	90607471
Oral discomfort	39.86	22.74	21	10598	10462	90607366
Polycythaemia	36.90	22.74	11	10608	1212	90616616
Aphonia	36.69	22.74	21	10598	12298	90605530
Infusion related reaction	34.92	22.74	4	10615	416776	90201052
Joint swelling	33.17	22.74	9	10610	503291	90114537
Nephrectomy	31.68	22.74	11	10608	1970	90615858
Drug hypersensitivity	31.10	22.74	8	10611	463601	90154227
Thyroiditis	28.49	22.74	12	10607	3625	90614203
Oligodipsia	28.46	22.74	5	10614	48	90617780
Feeding disorder	27.61	22.74	20	10599	17492	90600336
Sinusitis	27.03	22.74	4	10615	343084	90274744
Rheumatoid arthritis	26.86	22.74	5	10614	362609	90255219
Hyperkeratosis	26.69	22.74	14	10605	6914	90610914
Hepatotoxicity	25.30	22.74	29	10590	45813	90572015
Hypersensitivity	23.47	22.74	12	10607	454665	90163163
Hepatic function abnormal	23.41	22.74	28	10591	46260	90571568
Renal cancer	22.86	22.74	12	10607	5933	90611895

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
Neoplasm progression	1475.15	19.27	578	24781	28422	42567554
Dysphonia	1418.71	19.27	559	24800	27891	42568085
Diarrhoea	919.57	19.27	1237	24122	459612	42136364
Fatigue	705.05	19.27	1060	24299	434581	42161395
Hypertension	666.09	19.27	645	24714	166559	42429417
Disease progression	652.12	19.27	596	24763	143060	42452916
Death	503.78	19.27	954	24405	470231	42125745
Palmar-plantar erythrodysaesthesia syndrome	434.36	19.27	222	25137	20360	42575616
Decreased appetite	400.10	19.27	531	24828	192606	42403370
Blood pressure increased	393.02	19.27	387	24972	101541	42494435
Stomatitis	275.80	19.27	233	25126	50096	42545880
Oral pain	226.12	19.27	122	25237	12474	42583502
Aphonia	221.17	19.27	86	25273	4103	42591873
Drug ineffective	201.53	19.27	63	25296	630134	41965842
Hypothyroidism	178.65	19.27	150	25209	31934	42564042
Glossodynia	166.65	19.27	70	25289	4082	42591894
Weight decreased	141.86	19.27	353	25006	207595	42388381
Nausea	105.91	19.27	491	24868	396308	42199668
Proteinuria	101.01	19.27	94	25265	22889	42573087
Blister	97.55	19.27	100	25259	27390	42568586
Dry skin	84.68	19.27	123	25236	48215	42547761
Immune-mediated hepatic disorder	83.23	19.27	37	25322	2477	42593499
Febrile neutropenia	81.69	19.27	8	25351	185695	42410281
Neutropenia	79.39	19.27	12	25347	199419	42396557
Product dose omission in error	70.44	19.27	50	25309	8304	42587672
Drug interaction	69.72	19.27	36	25323	266963	42329013
Constipation	68.29	19.27	232	25127	162059	42433917
Second primary malignancy	66.52	19.27	51	25308	9524	42586452
Dry mouth	66.26	19.27	99	25260	39780	42556196
Asthenia	65.70	19.27	335	25024	280458	42315518
Oral discomfort	65.31	19.27	33	25326	2944	42593032
Thyroid disorder	64.62	19.27	36	25323	3914	42592062
Taste disorder	63.64	19.27	51	25308	10156	42585820
Blood pressure abnormal	58.21	19.27	48	25311	9950	42586026
Malignant neoplasm progression	57.54	19.27	168	25191	108232	42487744
Pain in extremity	57.04	19.27	208	25151	150396	42445580
Immune-mediated myocarditis	56.82	19.27	27	25332	2107	42593869
Toxicity to various agents	53.94	19.27	35	25324	229101	42366875
Overdose	50.59	19.27	3	25356	105261	42490715
Anaemia	48.81	19.27	57	25302	280221	42315755
Nephrectomy	45.68	19.27	18	25341	889	42595087
Product dose omission issue	44.63	19.27	196	25163	154169	42441807
Off label use	43.61	19.27	574	24785	637761	41958215
Pancytopenia	42.66	19.27	9	25350	117734	42478242
Headache	42.27	19.27	265	25094	239104	42356872
Pneumonia	40.68	19.27	123	25236	422026	42173950
Tongue discomfort	38.87	19.27	15	25344	700	42595276
Adrenal insufficiency	38.85	19.27	52	25307	18872	42577104
Body surface area decreased	38.79	19.27	7	25352	10	42595966
Blood thyroid stimulating hormone increased	38.55	19.27	29	25330	5263	42590713
Thrombocytopenia	36.08	19.27	36	25323	190243	42405733
Dehydration	35.78	19.27	173	25186	141594	42454382
Hyperkeratosis	33.25	19.27	25	25334	4533	42591443
Oropharyngeal pain	32.96	19.27	76	25283	42434	42553542
Thyroid function test abnormal	32.22	19.27	13	25346	683	42595293
Thyroiditis	31.11	19.27	21	25338	3215	42592761
Abdominal discomfort	31.07	19.27	107	25252	75148	42520828
Hepatic function abnormal	29.34	19.27	82	25277	51485	42544491
Arthralgia	28.91	19.27	215	25144	205023	42390953
Abdominal pain upper	28.65	19.27	111	25248	82498	42513478
Oral mucosal blistering	28.37	19.27	18	25341	2483	42593493
Nephritis	28.13	19.27	21	25338	3768	42592208
Cardiac arrest	28.09	19.27	15	25344	109305	42486671
Agitation	27.65	19.27	3	25356	64311	42531665
Ageusia	27.12	19.27	34	25325	11571	42584405
Therapy interrupted	27.09	19.27	48	25311	22202	42573774
Osteonecrosis of jaw	27.04	19.27	44	25315	19005	42576971
Multiple organ dysfunction syndrome	25.39	19.27	13	25346	97022	42498954
Condition aggravated	25.03	19.27	76	25283	260678	42335298
Drug hypersensitivity	25.00	19.27	14	25345	99375	42496601
Sepsis	24.65	19.27	51	25308	199283	42396693
Respiratory failure	24.55	19.27	24	25335	128108	42467868
Tachycardia	24.36	19.27	15	25344	101072	42494904
Asthma	24.19	19.27	4	25355	62310	42533666
Protein urine present	24.08	19.27	23	25336	5778	42590198
Pyrexia	24.03	19.27	137	25222	393905	42202071
Hepatic enzyme increased	22.40	19.27	69	25290	45715	42550261
Illness	22.06	19.27	47	25312	24883	42571093
Hyperaesthesia	21.73	19.27	22	25337	5930	42590046
Skin exfoliation	21.63	19.27	64	25295	41489	42554487
Tremor	21.19	19.27	16	25343	96913	42499063
Hypoxia	20.37	19.27	8	25351	69778	42526198
Hyperthyroidism	20.18	19.27	33	25326	14308	42581668
Renal impairment	20.00	19.27	123	25236	110105	42485871
Coronary artery disease	19.67	19.27	4	25355	53716	42542260
Rhabdomyolysis	19.61	19.27	11	25348	78008	42517968
Hepatotoxicity	19.51	19.27	45	25314	25122	42570854
Therapy non-responder	19.48	19.27	4	25355	53355	42542621
Incorrect dose administered	19.28	19.27	4	25355	52970	42543006

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Neoplasm progression	2185.06	20.25	802	33544	63793	110491160
Dysphonia	1561.80	20.25	658	33688	75271	110479682
Diarrhoea	1311.98	20.25	1677	32669	1137828	109417125
Death	1038.36	20.25	1174	33172	697695	109857258
Disease progression	942.17	20.25	702	33644	243332	110311621
Fatigue	857.25	20.25	1422	32924	1214536	109340417
Hypertension	784.61	20.25	874	33472	509210	110045743
Palmar-plantar erythrodysaesthesia syndrome	671.15	20.25	303	34043	40722	110514231
Decreased appetite	587.18	20.25	729	33617	475117	110079836
Blood pressure increased	574.77	20.25	541	33805	257832	110297121
Oral pain	325.14	20.25	180	34166	37264	110517689
Hypothyroidism	317.22	20.25	226	34120	72673	110482280
Stomatitis	264.03	20.25	370	33976	269872	110285081
Drug ineffective	256.06	20.25	78	34268	1520462	109034491
Aphonia	232.63	20.25	102	34244	12758	110542195
Weight decreased	230.82	20.25	472	33874	467585	110087368
Proteinuria	149.01	20.25	113	34233	39905	110515048
Nausea	146.54	20.25	762	33584	1234928	109320025
Constipation	135.59	20.25	325	34021	357461	110197492
Immune-mediated hepatic disorder	134.44	20.25	51	34295	4399	110550554
Dry skin	119.48	20.25	157	34189	107496	110447457
Malignant neoplasm progression	118.23	20.25	202	34144	174365	110380588
Asthenia	116.35	20.25	472	33874	688527	109866426
Second primary malignancy	102.35	20.25	66	34280	18002	110536951
Off label use	101.16	20.25	802	33544	1499383	109055570
Thyroid disorder	98.63	20.25	63	34283	16906	110538047
Product dose omission issue	93.76	20.25	265	34081	321517	110233436
Drug hypersensitivity	92.65	20.25	15	34331	454075	110100878
Dehydration	92.24	20.25	241	34105	279270	110275683
Product dose omission in error	91.09	20.25	68	34278	23444	110531509
Oral discomfort	88.99	20.25	51	34295	11260	110543693
Blood pressure abnormal	76.22	20.25	60	34286	22364	110532589
Immune-mediated myocarditis	73.99	20.25	31	34315	3467	110551486
Nephrectomy	71.69	20.25	28	34318	2612	110552341
Febrile neutropenia	70.42	20.25	8	34338	316759	110238194
Hepatic function abnormal	63.95	20.25	106	34240	89189	110465764
Wheezing	63.40	20.25	4	34342	255226	110299727
Hyperkeratosis	63.06	20.25	38	34308	9201	110545752
Joint swelling	62.02	20.25	30	34316	442815	110112138
Blood thyroid stimulating hormone increased	60.14	20.25	41	34305	12260	110542693
Arthropathy	59.74	20.25	9	34337	287513	110267440
Treatment failure	56.86	20.25	9	34337	277225	110277728
Thyroiditis	55.39	20.25	31	34315	6542	110548411
Asthma	53.96	20.25	7	34339	250284	110304669
Sinusitis	53.78	20.25	13	34333	296675	110258278
Adrenal insufficiency	53.60	20.25	66	34280	42324	110512629
Drug interaction	53.54	20.25	46	34300	500137	110054816
Neutropenia	51.51	20.25	26	34320	374594	110180359
Body surface area decreased	51.48	20.25	10	34336	59	110554894
Renal impairment	49.82	20.25	150	34196	188295	110366658
Overdose	49.30	20.25	7	34339	233787	110321166
Toxicity to various agents	49.26	20.25	46	34300	480509	110074444
Condition aggravated	48.48	20.25	97	34249	734739	109820214
Rheumatoid arthritis	47.24	20.25	17	34329	299596	110255357
Feeding disorder	45.90	20.25	44	34302	21318	110533635
Pain in extremity	45.78	20.25	283	34063	486835	110068118
Oral mucosal blistering	44.97	20.25	29	34317	7905	110547048
Posterior reversible encephalopathy syndrome	44.89	20.25	54	34292	33807	110521146
Hypersensitivity	44.64	20.25	36	34310	403962	110150991
Tongue discomfort	42.99	20.25	20	34326	2868	110552085
Pancytopenia	42.54	20.25	7	34339	209606	110345347
Osteoarthritis	42.15	20.25	4	34342	182619	110372334
Myocarditis	41.61	20.25	49	34297	30006	110524947
Skin exfoliation	41.36	20.25	87	34259	87564	110467389
Pericarditis	40.89	20.25	9	34337	219105	110335848
Dry mouth	39.31	20.25	144	34202	199804	110355149
Drug intolerance	38.13	20.25	42	34304	406470	110148483
Lower respiratory tract infection	37.97	20.25	14	34332	243092	110311861
Hyperthyroidism	37.71	20.25	46	34300	29215	110525738
Polycythaemia	37.64	20.25	19	34327	3256	110551697
Ageusia	37.62	20.25	38	34308	19607	110535346
Therapy non-responder	37.52	20.25	3	34343	157304	110397649
Protein urine present	37.46	20.25	30	34316	11454	110543499
Infusion related reaction	37.29	20.25	38	34308	381124	110173829
Irritable bowel syndrome	36.85	20.25	4	34342	164211	110390742
Weight increased	35.50	20.25	47	34299	419597	110135356
Pneumonia	34.90	20.25	147	34199	876567	109678386
Urticaria	34.49	20.25	29	34317	318828	110236125
Osteonecrosis of jaw	34.37	20.25	57	34289	47960	110506993
Renal cancer	34.15	20.25	30	34316	13004	110541949
Discomfort	34.15	20.25	12	34334	214695	110340258
Nasopharyngitis	33.52	20.25	44	34302	394317	110160636
Nephrotic syndrome	32.61	20.25	30	34316	13801	110541152
Leukopenia	32.45	20.25	4	34342	148787	110406166
Renal cell carcinoma	31.92	20.25	23	34323	7507	110547446
Myalgia	31.69	20.25	145	34201	222236	110332717
Thyroid function test abnormal	31.45	20.25	17	34329	3350	110551603
Hospice care	31.27	20.25	28	34318	12445	110542508
Taste disorder	30.96	20.25	65	34281	65322	110489631
Blister	30.02	20.25	145	34201	227231	110327722
Wound	29.70	20.25	18	34328	234419	110320534
Eating disorder	29.66	20.25	42	34304	30816	110524137
Depression	29.51	20.25	33	34313	317302	110237651
Dysgeusia	29.07	20.25	66	34280	69919	110485034
Swelling	28.99	20.25	40	34306	351001	110203952
Intentional product use issue	28.76	20.25	21	34325	247885	110307068
Oropharyngeal pain	27.92	20.25	99	34247	135177	110419776
Speech disorder	27.76	20.25	60	34286	61509	110493444
Blood corticotrophin increased	27.43	20.25	8	34338	303	110554650
Cancer pain	27.15	20.25	20	34326	6752	110548201
Blood cholesterol increased	26.64	20.25	12	34334	184773	110370180
Musculoskeletal stiffness	26.13	20.25	29	34317	279793	110275160
Type 1 diabetes mellitus	26.09	20.25	22	34324	9025	110545928
Hyperaesthesia	25.52	20.25	27	34319	14700	110540253
Immune-mediated hepatitis	25.08	20.25	19	34327	6692	110548261
Injury	24.80	20.25	12	34334	177253	110377700
Metastatic renal cell carcinoma	24.51	20.25	13	34333	2467	110552486
Pyrexia	24.45	20.25	171	34175	898094	109656859
Oligodipsia	24.41	20.25	5	34341	40	110554913
Oedema	24.07	20.25	18	34328	209958	110344995
Illness	23.22	20.25	67	34279	82104	110472849
Bronchitis	22.95	20.25	10	34336	157022	110397931
Ill-defined disorder	22.90	20.25	10	34336	156843	110398110
Tachycardia	22.84	20.25	22	34324	226623	110328330
Anaphylactic reaction	22.78	20.25	4	34342	114296	110440657
Immune-mediated hypothyroidism	22.71	20.25	13	34333	2862	110552091
Medication error	22.57	20.25	3	34343	105363	110449590
Agitation	22.44	20.25	4	34342	113047	110441906
Nephritis	22.14	20.25	17	34329	6109	110548844
Glossitis	22.00	20.25	15	34331	4486	110550467
Cardiac dysfunction	21.90	20.25	17	34329	6206	110548747
Hepatic cytolysis	21.85	20.25	51	34295	55002	110499951
Mobility decreased	21.73	20.25	25	34321	237397	110317556
Liver injury	21.32	20.25	10	34336	150403	110404550
Gastrointestinal perforation	21.23	20.25	18	34328	7438	110547515
Cardiac arrest	21.13	20.25	18	34328	196735	110358218
Dental care	20.87	20.25	9	34337	1080	110553873
Alopecia	20.85	20.25	52	34294	364701	110190252
Angioedema	20.64	20.25	3	34343	98497	110456456
Immune-mediated renal disorder	20.56	20.25	8	34338	739	110554214
Inflammation	20.36	20.25	18	34328	193220	110361733

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EK01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors
FDA MoA	N0000020000	Receptor Tyrosine Kinase Inhibitors
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D047428	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
CHEBI has role	CHEBI:35610	antineoplastic agent
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitor
CHEBI has role	CHEBI:65207	vascular endothelial growth factor receptor antagonist

Related Drugs by ATC class:

L01EK Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors 3 drugs

apatinibfruquintinibtivozanib

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

Disease	Relation	SNOMED_ID	DOID
Renal cell carcinoma	indication	702391001	DOID:4450

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.57	acidic
pKa2	12.18	acidic
pKa3	4.85	Basic
pKa4	1.98	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
1MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	10570202	Feb. 3, 2035	IN COMBINATION WITH PEMBROLIZUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
1MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	12534530	Feb. 3, 2035	A FIRST-LINE METHOD OF TREATING ADVANCED RENAL CELL CARCINOMA IN AN INDIVIDUAL BY ADMINISTERING AXITINIB AT A STARTING DOSE OF 5 MG TWICE DAILY IN COMBINATION WITH PEMBROLIZUMAB, WHERE THE AXITINIB DOSE IS INCREASED AS CLAIMED
1MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	12534530	Feb. 3, 2035	A FIRST-LINE METHOD OF TREATING ADVANCED RENAL CELL CARCINOMA IN AN INDIVIDUAL BY ADMINISTERING AXITINIB AT A STARTING DOSE OF 5 MG TWICE DAILY IN COMBINATION WITH PEMBROLIZUMAB, WHERE THE AXITINIB DOSE IS REDUCED AS CLAIMED
5MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	10570202	Feb. 3, 2035	IN COMBINATION WITH PEMBROLIZUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
5MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	12534530	Feb. 3, 2035	A FIRST-LINE METHOD OF TREATING ADVANCED RENAL CELL CARCINOMA IN AN INDIVIDUAL BY ADMINISTERING AXITINIB AT A STARTING DOSE OF 5 MG TWICE DAILY IN COMBINATION WITH PEMBROLIZUMAB, WHERE THE AXITINIB DOSE IS INCREASED AS CLAIMED
5MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	12534530	Feb. 3, 2035	A FIRST-LINE METHOD OF TREATING ADVANCED RENAL CELL CARCINOMA IN AN INDIVIDUAL BY ADMINISTERING AXITINIB AT A STARTING DOSE OF 5 MG TWICE DAILY IN COMBINATION WITH PEMBROLIZUMAB, WHERE THE AXITINIB DOSE IS REDUCED AS CLAIMED
1MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	10869924	Jan. 12, 2037	AXITINIB IN COMBINATION WITH AVELUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA
5MG	INLYTA	PF PRISM CV	N202324	Jan. 27, 2012	RX	TABLET	ORAL	10869924	Jan. 12, 2037	AXITINIB IN COMBINATION WITH AVELUMAB FOR THE FIRST-LINE TREATMENT OF PATIENTS WITH ADVANCED RENAL CELL CARCINOMA

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
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	Kd	8.23		CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN	INHIBITOR	Kd	6.77		CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN	INHIBITOR	Kd	8.24		CHEMBL	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		Kd	9.31		CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		Kd	5.64		CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN		Kd	6.73		CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN		Kd	5.57		CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	5.57		CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	7.51		CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	7		CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN		Kd	7.68		CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN		Kd	9.29		CHEMBL
Histone deacetylase 6	Enzyme	Q9UBN7	HDAC6_HUMAN		IC50	6.39		CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	5.41		CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN		Kd	6.68		CHEMBL
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	5.96		CHEMBL
High affinity nerve growth factor receptor	Kinase	P04629	NTRK1_HUMAN		Kd	5.74		CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	5.48		CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle	Kinase	Q9H1R3	MYLK2_HUMAN		Kd	5.89		CHEMBL
Tyrosine-protein kinase CSK	Kinase	P41240	CSK_HUMAN		Kd	5.96		CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	6.51		CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	5.92		CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN		Kd	6.09		CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN		Kd	6.42		CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	5.92		CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Ki	8.38		CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	8.89		CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	6.43		CHEMBL
Dual specificity protein kinase TTK	Kinase	P33981	TTK_HUMAN		Kd	5.41		CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	7.15		CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		Kd	6.96		CHEMBL
TRAF2 and NCK-interacting protein kinase	Kinase	Q9UKE5	TNIK_HUMAN		Kd	6.74		CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	5.74		CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		Kd	7.14		CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	6		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5	Kinase	Q9Y4K4	M4K5_HUMAN		Kd	6.26		CHEMBL
Mitogen-activated protein kinase kinase kinase 4	Kinase	Q9Y6R4	M3K4_HUMAN		Kd	5.25		CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	5.57		CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	5		CHEMBL
Cyclin-dependent kinase 16	Kinase	Q00536	CDK16_HUMAN		Kd	5.28		CHEMBL
Serine/threonine-protein kinase 4	Kinase	Q13043	STK4_HUMAN		Kd	5.85		CHEMBL
Activated CDC42 kinase 1	Kinase	Q07912	ACK1_HUMAN		Kd	5.22		CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	6		CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 2	Kinase	Q96RR4	KKCC2_HUMAN		Kd	5.82		CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1	Kinase	Q8N5S9	KKCC1_HUMAN		Kd	5.85		CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	6.47		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 1	Kinase	Q02750	MP2K1_HUMAN		Kd	5.57		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 2	Kinase	P36507	MP2K2_HUMAN		Kd	5.59		CHEMBL
Tyrosine-protein kinase ITK/TSK	Kinase	Q08881	ITK_HUMAN		Kd	5.92		CHEMBL
Tyrosine-protein kinase receptor UFO	Kinase	P30530	UFO_HUMAN		Kd	6.38		CHEMBL
Serine/threonine-protein kinase N2	Kinase	Q16513	PKN2_HUMAN		Kd	5.57		CHEMBL
Serine/threonine-protein kinase 3	Kinase	Q13188	STK3_HUMAN		Kd	5.66		CHEMBL
NUAK family SNF1-like kinase 2	Kinase	Q9H093	NUAK2_HUMAN		Kd	5.89		CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.80		CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	5.44		CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	5.59		CHEMBL
Serine/threonine-protein kinase RIO1	Kinase	Q9BRS2	RIOK1_HUMAN		Kd	5.92		CHEMBL
Tyrosine-protein kinase receptor Tie-1	Kinase	P35590	TIE1_HUMAN		Kd	7.01		CHEMBL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN		Kd	5.62		CHEMBL
Casein kinase II subunit alpha'	Kinase	P19784	CSK22_HUMAN		Kd	5.55		CHEMBL
Serine/threonine-protein kinase RIO3	Kinase	O14730	RIOK3_HUMAN		Kd	6		CHEMBL
SRSF protein kinase 1	Kinase	Q96SB4	SRPK1_HUMAN		Kd	5.74		CHEMBL
Activin receptor type-2B	Kinase	Q13705	AVR2B_HUMAN		Kd	5.28		CHEMBL
Ankyrin repeat and protein kinase domain-containing protein 1	Kinase	Q8NFD2	ANKK1_HUMAN		Kd	5.44		CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	5.28		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	6.48		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	5.92		CHEMBL
Aurora kinase B	Kinase	Q96GD4	AURKB_HUMAN		Kd	7.96		CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	5.51		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	6.46		CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN		Kd	5.49		CHEMBL
Mitogen-activated protein kinase kinase kinase 9	Kinase	P80192	M3K9_HUMAN		Kd	5.52		CHEMBL
Serine/threonine-protein kinase MRCK beta	Kinase	Q9Y5S2	MRCKB_HUMAN		Kd	5.32		CHEMBL
Myosin-IIIa	Kinase	Q8NEV4	MYO3A_HUMAN		Kd	5.72		CHEMBL
Serine/threonine-protein kinase PAK 4	Kinase	O96013	PAK4_HUMAN		Kd	5.35		CHEMBL
Serine/threonine-protein kinase SIK1	Kinase	P57059	SIK1_HUMAN		Kd	5.68		CHEMBL
Dual specificity testis-specific protein kinase 1	Kinase	Q15569	TESK1_HUMAN		Kd	5.37		CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase	Kinase	P19525	E2AK2_HUMAN		Kd	5.13		CHEMBL
Receptor-interacting serine/threonine-protein kinase 1	Kinase	Q13546	RIPK1_HUMAN		Kd	5.60		CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		Kd	5.49		CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	5.89		CHEMBL
Misshapen-like kinase 1	Kinase	Q8N4C8	MINK1_HUMAN		Kd	6.25		CHEMBL
Cyclin-dependent kinase-like 2	Kinase	Q92772	CDKL2_HUMAN		Kd	6.28		CHEMBL
Protein delta homolog 1	Membrane other	P80370	DLK1_HUMAN		Kd	5.77		CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	6.44		CHEMBL
G protein-coupled receptor kinase 4	Kinase	P32298	GRK4_HUMAN		Kd	5.64		CHEMBL
Hormonally up-regulated neu tumor-associated kinase	Kinase	P57058	HUNK_HUMAN		Kd	5.82		CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	5.51		CHEMBL
Mitogen-activated protein kinase kinase kinase 3	Kinase	Q99759	M3K3_HUMAN		Kd	5.55		CHEMBL
SRSF protein kinase 3	Kinase	Q9UPE1	SRPK3_HUMAN		Kd	5.64		CHEMBL
Serine/threonine-protein kinase ULK2	Kinase	Q8IYT8	ULK2_HUMAN		Kd	5		CHEMBL
Serine/threonine-protein kinase ULK3	Kinase	Q6PHR2	ULK3_HUMAN		Kd	6.17		CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	6.57		CHEMBL
Receptor-interacting serine/threonine-protein kinase 4	Kinase	P57078	RIPK4_HUMAN		Kd	5.85		CHEMBL
Bone morphogenetic protein receptor type-1B	Kinase	O00238	BMR1B_HUMAN		Kd	5.54		CHEMBL
Mitogen-activated protein kinase kinase kinase 12	Kinase	Q12852	M3K12_HUMAN		Kd	5.77		CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	6.85		CHEMBL
Myosin light chain kinase 3	Kinase	Q32MK0	MYLK3_HUMAN		Kd	5.77		CHEMBL
Leucine-rich repeat serine/threonine-protein kinase 2	Kinase	Q5S007	LRRK2_HUMAN		Kd	6.04		CHEMBL
Ferrochelatase, mitochondrial	Enzyme	P22830	HEMH_HUMAN		Kd	5.17		CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	5.51		CHEMBL
Uncharacterized protein FLJ45252	Unclassified	Q6ZSR9	YJ005_HUMAN		Kd	5.64		CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		Kd	9.24		CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	8.82		CHEMBL

External reference:

ID	Source
4031332	VUID
N0000184323	NUI
D03218	KEGG_DRUG
4031332	VANDF
C1700874	UMLSCUI
CHEBI:66910	CHEBI
AXI	PDB_CHEM_ID
CHEMBL1289926	ChEMBL_ID
D000077784	MESH_DESCRIPTOR_UI
DB06626	DRUGBANK_ID
5659	IUPHAR_LIGAND_ID
8720	INN_ID
C9LVQ0YUXG	UNII
6450551	PUBCHEM_CID
1242999	RXNORM
187097	MMSL
28294	MMSL
d07823	MMSL
014143	NDDF
427882000	SNOMEDCT_US
429507005	SNOMEDCT_US
C9LVQ0YUXG	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0145	TABLET, FILM COATED	1 mg	ORAL	NDA	29 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	0069-0151	TABLET, FILM COATED	5 mg	ORAL	NDA	29 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	63539-026	TABLET, FILM COATED	1 mg	ORAL	NDA	29 sections
INLYTA	HUMAN PRESCRIPTION DRUG LABEL	1	63539-044	TABLET, FILM COATED	5 mg	ORAL	NDA	29 sections