pazopanib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
angiogenesis inhibitors	4118	444731-52-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: GW786034B pazopanib votrient GW 786034 pazopanib hydrochloride pazopanib HCl	Pazopanib is a multi-tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-α and -β, fibroblast growth factor receptor (FGFR)-1 and -3, cytokine receptor (Kit), interleukin-2 receptor-inducible T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck), and transmembrane glycoprotein receptor tyrosine kinase (c-Fms). In vitro, pazopanib inhibited ligand-induced autophosphorylation of VEGFR-2, Kit, and PDGFR-β receptors. In vivo, pazopanib inhibited VEGF-induced VEGFR-2 phosphorylation in mouse lungs, angiogenesis in a mouse model, and the growth of some human tumor xenografts in mice. Molecular weight: 437.52 Formula: C21H23N7O2S CLOGP: 3.50 LIPINSKI: 0 HAC: 9 HDO: 2 TPSA: 119.03 ALOGS: -4 ROTB: 5 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

GW786034B
pazopanib
votrient
GW 786034
pazopanib hydrochloride
pazopanib HCl

Pazopanib is a multi-tyrosine kinase inhibitor of vascular endothelial growth factor receptor (VEGFR)-1, VEGFR-2, VEGFR-3, platelet-derived growth factor receptor (PDGFR)-α and -β, fibroblast growth factor receptor (FGFR)-1 and -3, cytokine receptor (Kit), interleukin-2 receptor-inducible T-cell kinase (Itk), leukocyte-specific protein tyrosine kinase (Lck), and transmembrane glycoprotein receptor tyrosine kinase (c-Fms). In vitro, pazopanib inhibited ligand-induced autophosphorylation of VEGFR-2, Kit, and PDGFR-β receptors. In vivo, pazopanib inhibited VEGF-induced VEGFR-2 phosphorylation in mouse lungs, angiogenesis in a mouse model, and the growth of some human tumor xenografts in mice.

Molecular weight: 437.52
Formula: C21H23N7O2S
CLOGP: 3.50
LIPINSKI: 0
HAC: 9
HDO: 2
TPSA: 119.03
ALOGS: -4
ROTB: 5

Status: ONP

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

Drug dosage:

Dose	Unit	Route
0.80	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution)	0.16 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	0.06 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
June 14, 2010	EMA
Oct. 19, 2009	FDA	NOVARTIS PHARMS CORP

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
Malignant neoplasm progression	775.09	22.04	362	12471	81759	63394430
Hair colour changes	484.57	22.04	115	12718	3012	63473177
Death	451.73	22.04	460	12373	373921	63102268
Diarrhoea	382.10	22.04	583	12250	714783	62761406
Hypertension	244.83	22.04	291	12542	279012	63197177
Nausea	155.72	22.04	449	12384	854022	62622167
Disease progression	150.77	22.04	153	12680	122605	63353584
Product use in unapproved indication	150.59	22.04	183	12650	178897	63297292
Decreased appetite	135.73	22.04	207	12626	250845	63225344
Fatigue	125.87	22.04	428	12405	887600	62588589
Hepatic function abnormal	124.17	22.04	83	12750	37059	63439130
Palmar-plantar erythrodysaesthesia syndrome	105.95	22.04	63	12770	22952	63453237
Desmoplastic small round cell tumour	105.02	22.04	18	12815	78	63476111
Metastases to lung	103.91	22.04	51	12782	12699	63463490
Metastases to peritoneum	83.65	22.04	30	12803	3412	63472777
Metastases to liver	72.26	22.04	50	12783	23589	63452600
Hypothyroidism	67.11	22.04	61	12772	42571	63433618
Vomiting	62.92	22.04	251	12582	559366	62916823
Jaundice	58.50	22.04	48	12785	29203	63446986
Blood bilirubin increased	58.17	22.04	53	12780	37087	63439102
Alanine aminotransferase increased	57.91	22.04	87	12746	103683	63372506
Blood pressure increased	57.46	22.04	111	12722	161951	63314238
Aspartate aminotransferase increased	55.16	22.04	79	12754	90198	63385991
Dysgeusia	55.01	22.04	57	12776	46653	63429536
Metastases to lymph nodes	52.97	22.04	28	12805	8130	63468059
Posterior reversible encephalopathy syndrome	51.39	22.04	36	12797	17309	63458880
Drug hypersensitivity	50.82	22.04	3	12830	310684	63165505
Transaminases increased	49.59	22.04	45	12788	31322	63444867
Metastases to pancreas	46.42	22.04	11	12822	285	63475904
Proteinuria	45.98	22.04	35	12798	19110	63457079
Ascites	44.92	22.04	48	12785	40680	63435509
Blood thyroid stimulating hormone increased	41.98	22.04	23	12810	7171	63469018
Pneumothorax	41.88	22.04	31	12802	16230	63459959
Ageusia	41.86	22.04	29	12804	13699	63462490
Hepatotoxicity	41.46	22.04	44	12789	36997	63439192
Metastases to central nervous system	40.70	22.04	28	12805	13077	63463112
Condition aggravated	39.46	22.04	16	12817	402201	63073988
Hypertensive crisis	39.05	22.04	29	12804	15257	63460932
Joint swelling	37.45	22.04	10	12823	327656	63148533
Neoplasm progression	36.81	22.04	41	12792	36387	63439802
Hypersensitivity	35.26	22.04	8	12825	292677	63183512
Peripheral artery haematoma	32.96	22.04	6	12827	39	63476150
Sinusitis	32.13	22.04	4	12829	226649	63249540
Asthenia	30.84	22.04	156	12677	383448	63092741
Neurofibrosarcoma	30.50	22.04	7	12826	157	63476032
Intestinal transit time abnormal	29.82	22.04	6	12827	70	63476119
Treatment failure	29.50	22.04	3	12830	199040	63277149
Cell death	29.24	22.04	13	12820	2588	63473601
Hyperthyroidism	29.16	22.04	24	12809	14649	63461540
Platelet count decreased	28.96	22.04	69	12764	116053	63360136
Pleural effusion	27.25	22.04	59	12774	93151	63383038
Left ventricular dysfunction	26.79	22.04	21	12812	11967	63464222
Tumour pain	25.68	22.04	10	12823	1427	63474762
Nephrotic syndrome	24.96	22.04	15	12818	5561	63470628
Concomitant disease aggravated	24.89	22.04	18	12815	9094	63467095
Thrombocytopenia	24.81	22.04	77	12756	151080	63325109
Amylase increased	23.18	22.04	15	12818	6330	63469859
Liver disorder	23.07	22.04	40	12793	53647	63422542
Weight increased	23.02	22.04	12	12821	260780	63215409
Dehydration	22.85	22.04	82	12751	173272	63302917
Wound	22.84	22.04	3	12830	163260	63312929
Cardiac failure	22.25	22.04	53	12780	89089	63387100

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
Hair colour changes	878.86	18.36	204	18802	1673	34936252
Malignant neoplasm progression	771.76	18.36	519	18487	87527	34850398
Diarrhoea	595.11	18.36	879	18127	389033	34548892
Death	368.70	18.36	720	18286	397329	34540596
Decreased appetite	274.18	18.36	391	18615	166001	34771924
Fatigue	229.93	18.36	572	18434	370081	34567844
Metastases to lung	212.55	18.36	103	18903	9217	34928708
Hypertension	203.22	18.36	306	18700	136137	34801788
Palmar-plantar erythrodysaesthesia syndrome	180.69	18.36	113	18893	16682	34921243
Nausea	168.20	18.36	483	18523	339425	34598500
Disease progression	154.52	18.36	238	18768	107839	34830086
Dysgeusia	138.56	18.36	115	18891	26382	34911543
Hypothyroidism	87.61	18.36	80	18926	20822	34917103
Pneumothorax	79.87	18.36	73	18933	19019	34918906
Product use in unapproved indication	78.13	18.36	187	18819	117312	34820613
Metastases to bone	75.45	18.36	58	18948	11912	34926013
Off label use	68.08	18.36	77	18929	419447	34518478
Blood pressure increased	65.99	18.36	147	18859	87955	34849970
Hepatic enzyme increased	65.68	18.36	93	18913	38987	34898938
Metastases to central nervous system	63.51	18.36	45	18961	8160	34929765
Proteinuria	62.32	18.36	63	18943	18579	34919346
Soft tissue sarcoma	61.64	18.36	13	18993	64	34937861
Weight decreased	61.57	18.36	223	18783	176078	34761847
Jaundice	59.79	18.36	80	18926	31802	34906123
Ageusia	58.60	18.36	47	18959	10261	34927664
Blood thyroid stimulating hormone increased	57.05	18.36	33	18973	4222	34933703
Hepatic function abnormal	52.74	18.36	90	18916	44273	34893652
Vomiting	50.91	18.36	267	18739	247354	34690571
Metastases to liver	49.03	18.36	48	18958	13615	34924310
Metastatic renal cell carcinoma	47.63	18.36	23	18983	2038	34935887
Therapy cessation	47.18	18.36	52	18954	16921	34921004
Blood bilirubin increased	45.92	18.36	78	18928	38218	34899707
Tumour pain	43.93	18.36	18	18988	1079	34936846
Alanine aminotransferase increased	43.65	18.36	119	18887	80696	34857229
Hypotension	42.43	18.36	35	18971	221614	34716311
Nephrotic syndrome	40.87	18.36	33	18973	7270	34930655
Neoplasm progression	39.95	18.36	56	18950	23244	34914681
Skin depigmentation	39.30	18.36	13	18993	423	34937502
Metastases to lymph nodes	39.08	18.36	27	18979	4701	34933224
Abdominal pain upper	38.33	18.36	105	18901	71385	34866540
Synovial sarcoma metastatic	37.31	18.36	7	18999	16	34937909
Stomatitis	36.46	18.36	75	18931	42439	34895486
Hepatotoxicity	34.42	18.36	50	18956	21435	34916490
Liver function test increased	34.37	18.36	41	18965	14524	34923401
Taste disorder	33.16	18.36	29	18977	7126	34930799
Activated partial thromboplastin time abnormal	33.13	18.36	9	18997	146	34937779
Pulmonary necrosis	33.05	18.36	11	18995	365	34937560
Renal cancer metastatic	32.98	18.36	12	18994	521	34937404
Condition aggravated	32.45	18.36	34	18972	192162	34745763
Fall	31.95	18.36	38	18968	202847	34735078
Osteoma	31.16	18.36	8	18998	103	34937822
Polycystic liver disease	31.09	18.36	8	18998	104	34937821
Toxicity to various agents	31.05	18.36	38	18968	200324	34737601
Osteonecrosis of jaw	30.67	18.36	43	18963	17846	34920079
Splenic necrosis	30.28	18.36	8	18998	116	34937809
Febrile neutropenia	29.55	18.36	19	18987	136830	34801095
Haemoglobin urine present	29.55	18.36	8	18998	128	34937797
Splenic cyst	29.43	18.36	8	18998	130	34937795
Asthenia	28.98	18.36	230	18776	245021	34692904
Neoplasm recurrence	28.98	18.36	17	18989	2232	34935693
Renal cell carcinoma	28.65	18.36	23	18983	5025	34932900
Liver disorder	28.04	18.36	58	18948	32939	34904986
Metastases to soft tissue	27.66	18.36	10	18996	426	34937499
Renal cancer	27.42	18.36	27	18979	7708	34930217
Aspartate aminotransferase increased	27.29	18.36	90	18916	67693	34870232
Drug interaction	27.15	18.36	51	18955	225895	34712030
Skin hypopigmentation	27.09	18.36	9	18997	297	34937628
Overdose	26.97	18.36	8	18998	91051	34846874
Metastases to adrenals	25.54	18.36	12	18994	1000	34936925
Sepsis	25.36	18.36	32	18974	166529	34771396
Dysphonia	24.62	18.36	45	18961	23338	34914587
Blood alkaline phosphatase increased	24.41	18.36	53	18953	31122	34906803
Splenic lesion	24.22	18.36	8	18998	259	34937666
Pleural effusion	24.14	18.36	98	18908	81448	34856477
Drug hypersensitivity	23.99	18.36	7	18999	80522	34857403
Urinary sediment present	23.55	18.36	8	18998	283	34937642
Second primary malignancy	23.38	18.36	25	18981	7861	34930064
Abdominal discomfort	22.80	18.36	78	18928	59757	34878168
Eyelash discolouration	22.41	18.36	4	19002	6	34937919
Intestinal perforation	22.19	18.36	26	18980	9034	34928891
Somnolence	21.91	18.36	17	18989	111099	34826826
Lordosis	21.88	18.36	8	18998	352	34937573
Faeces pale	21.83	18.36	12	18994	1391	34936534
Glossodynia	21.33	18.36	17	18989	3676	34934249
Red blood cell abnormality	20.98	18.36	8	18998	396	34937529
COVID-19	20.90	18.36	8	18998	77542	34860383
Pneumonia	20.89	18.36	114	18892	362513	34575412
Tremor	19.92	18.36	10	18996	82577	34855348
Malignant connective tissue neoplasm	19.55	18.36	3	19003	0	34937925
Oxygen saturation decreased	19.45	18.36	3	19003	53815	34884110
Impaired healing	19.39	18.36	32	18974	15302	34922623
Pulmonary mass	19.34	18.36	29	18977	12783	34925142
Disseminated intravascular coagulation	19.30	18.36	39	18967	21777	34916148
Recurrent cancer	19.24	18.36	11	18995	1376	34936549
Hyperthyroidism	19.01	18.36	26	18980	10540	34927385
Blood bilirubin abnormal	19.01	18.36	9	18997	763	34937162
Gamma-glutamyltransferase increased	18.80	18.36	46	18960	29185	34908740

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
Malignant neoplasm progression	1193.58	17.84	648	23233	135342	79585165
Hair colour changes	748.90	17.84	187	23694	4045	79716462
Death	631.45	17.84	808	23073	565706	79154801
Diarrhoea	505.11	17.84	922	22959	879567	78840940
Hypertension	344.82	17.84	458	23423	330534	79389973
Disease progression	279.72	17.84	309	23572	184053	79536454
Metastases to lung	275.72	17.84	126	23755	18037	79702470
Decreased appetite	269.77	17.84	415	23466	342003	79378504
Palmar-plantar erythrodysaesthesia syndrome	219.85	17.84	132	23749	33002	79687505
Fatigue	174.74	17.84	641	23240	929086	78791421
Hepatic function abnormal	158.98	17.84	149	23732	72958	79647549
Nausea	148.89	17.84	622	23259	956574	78763933
Hypothyroidism	118.15	17.84	109	23772	52283	79668224
Metastases to liver	110.39	17.84	81	23800	28233	79692274
Pneumothorax	110.37	17.84	81	23800	28242	79692265
Jaundice	105.09	17.84	103	23778	53246	79667261
Product use in unapproved indication	104.42	17.84	231	23650	250128	79470379
Proteinuria	100.47	17.84	81	23800	32421	79688086
Metastases to lymph nodes	100.40	17.84	53	23828	10344	79710163
Blood bilirubin increased	98.44	17.84	110	23771	66122	79654385
Desmoplastic small round cell tumour	95.34	17.84	18	23863	93	79720414
Metastases to central nervous system	87.78	17.84	57	23824	16318	79704189
Alanine aminotransferase increased	82.93	17.84	163	23718	162407	79558100
Metastases to peritoneum	78.07	17.84	34	23847	4338	79716169
Dysgeusia	76.58	17.84	90	23791	57087	79663420
Blood thyroid stimulating hormone increased	75.78	17.84	43	23838	9665	79710842
Hepatotoxicity	72.40	17.84	83	23798	51269	79669238
Drug hypersensitivity	70.24	17.84	5	23876	298911	79421596
Therapy cessation	67.48	17.84	69	23812	37493	79683014
Metastases to bone	67.39	17.84	57	23824	24370	79696137
Aspartate aminotransferase increased	65.89	17.84	135	23746	138506	79582001
Metastatic renal cell carcinoma	64.92	17.84	25	23856	2330	79718177
Neoplasm progression	63.71	17.84	78	23803	51604	79668903
Blood pressure increased	63.49	17.84	172	23709	211188	79509319
Vomiting	61.91	17.84	375	23506	665453	79055054
Condition aggravated	56.12	17.84	41	23840	501083	79219424
Ageusia	54.70	17.84	43	23838	16589	79703918
Nephrotic syndrome	52.89	17.84	36	23845	11138	79709369
Hyperthyroidism	47.72	17.84	45	23836	22164	79698343
Hypertensive crisis	46.39	17.84	43	23838	20727	79699780
Soft tissue sarcoma	45.93	17.84	11	23870	198	79720309
Joint swelling	45.28	17.84	15	23866	288631	79431876
Fall	44.83	17.84	48	23833	487581	79232926
Tumour pain	44.73	17.84	19	23862	2280	79718227
Pleural effusion	43.37	17.84	118	23763	145144	79575363
Asthenia	42.36	17.84	280	23601	511409	79209098
Weight decreased	41.51	17.84	213	23668	354985	79365522
Off label use	38.57	17.84	141	23740	907074	78813433
Platelet count decreased	38.49	17.84	137	23744	194527	79525980
Transaminases increased	38.13	17.84	61	23820	51682	79668825
Osteonecrosis of jaw	36.11	17.84	54	23827	43172	79677335
Pulmonary mass	36.07	17.84	44	23837	28990	79691517
Overdose	35.90	17.84	6	23875	184200	79536307
Pulmonary necrosis	35.79	17.84	11	23870	519	79719988
Osteoma	35.55	17.84	8	23873	108	79720399
Hypotension	35.50	17.84	48	23833	440269	79280238
Retro-orbital neoplasm	35.26	17.84	7	23874	49	79720458
Therapeutic product effect decreased	35.09	17.84	4	23877	163859	79556648
Renal cancer	34.69	17.84	29	23852	12197	79708310
Neoplasm recurrence	33.79	17.84	19	23862	4195	79716312
Liver disorder	33.76	17.84	70	23811	72347	79648160
Disseminated intravascular coagulation	33.17	17.84	47	23834	35795	79684712
Ejection fraction decreased	32.98	17.84	46	23835	34531	79685976
Polycystic liver disease	32.37	17.84	8	23873	165	79720342
Splenic necrosis	32.10	17.84	8	23873	171	79720336
Hyperbilirubinaemia	31.83	17.84	38	23843	24480	79696027
Activated partial thromboplastin time abnormal	31.28	17.84	9	23872	337	79720170
COVID-19	31.03	17.84	5	23876	157669	79562838
Sinusitis	30.92	17.84	10	23871	195491	79525016
Renal cell carcinoma	30.68	17.84	21	23860	6557	79713950
Neurofibrosarcoma	30.32	17.84	8	23873	216	79720291
Metastases to soft tissue	30.23	17.84	10	23871	599	79719908
Urticaria	30.14	17.84	9	23872	185192	79535315
Hypersensitivity	29.90	17.84	21	23860	262218	79458289
Metastasis	29.82	17.84	21	23860	6859	79713648
Posterior reversible encephalopathy syndrome	29.72	17.84	38	23843	26243	79694264
Liver function test increased	29.45	17.84	47	23834	39726	79680781
Musculoskeletal stiffness	29.41	17.84	8	23873	175000	79545507
Splenic cyst	29.02	17.84	8	23873	256	79720251
Synovial sarcoma metastatic	28.40	17.84	5	23876	16	79720491
Ascites	28.40	17.84	67	23814	75495	79645012
Weight increased	28.12	17.84	25	23856	277361	79443146
Hepatic mass	28.01	17.84	14	23867	2437	79718070
Blood alkaline phosphatase increased	27.89	17.84	60	23821	63604	79656903
Intestinal transit time abnormal	27.47	17.84	6	23875	70	79720437
Renal impairment	26.97	17.84	106	23775	157677	79562830
Nasopharyngitis	26.81	17.84	22	23859	253859	79466648
Cardiac failure	26.44	17.84	104	23777	154738	79565769
Drug-induced liver injury	26.35	17.84	60	23821	66057	79654450
Arthralgia	26.16	17.84	86	23795	571717	79148790
Hepatic enzyme increased	26.00	17.84	116	23765	182494	79538013
Polycythaemia	25.97	17.84	13	23868	2271	79718236
Skin hypopigmentation	25.43	17.84	10	23871	985	79719522
Hepatic lesion	25.08	17.84	19	23862	6940	79713567
Tumour necrosis	25.03	17.84	12	23869	1910	79718597
Lordosis	24.79	17.84	8	23873	443	79720064
Thyroid function test abnormal	24.78	17.84	14	23867	3120	79717387
Renal cancer metastatic	24.67	17.84	9	23872	722	79719785
Prostatic specific antigen abnormal	24.62	17.84	8	23873	453	79720054
Gamma-glutamyltransferase increased	24.49	17.84	52	23829	54628	79665879
Peripheral artery haematoma	24.22	17.84	6	23875	125	79720382
Depression	23.88	17.84	18	23863	216772	79503735
Second primary malignancy	23.33	17.84	25	23856	14325	79706182
Treatment failure	23.20	17.84	11	23870	170475	79550032
Asthma	23.03	17.84	6	23875	135089	79585418
Thrombocytopenia	23.01	17.84	147	23734	265112	79455395
Splenic lesion	22.84	17.84	8	23873	570	79719937
Metastases to pancreas	22.81	17.84	8	23873	572	79719935
Mucosal inflammation	22.14	17.84	61	23820	75519	79644988
Bronchitis	21.90	17.84	6	23875	130638	79589869
Malignant connective tissue neoplasm	21.34	17.84	3	23878	0	79720507
Dehydration	21.19	17.84	137	23744	248050	79472457
Skin depigmentation	21.02	17.84	9	23872	1101	79719406
Intestinal perforation	20.98	17.84	26	23855	17400	79703107
Amylase increased	20.87	17.84	21	23860	11188	79709319
Loss of personal independence in daily activities	20.76	17.84	3	23878	102577	79617930
Red blood cell abnormality	20.69	17.84	8	23873	754	79719753
Metastases to spine	20.63	17.84	14	23867	4310	79716197
Muscle mass	20.58	17.84	7	23874	457	79720050
Left ventricular dysfunction	20.34	17.84	27	23854	19334	79701173
Renal cancer recurrent	20.33	17.84	5	23876	101	79720406
Metastases to adrenals	19.46	17.84	9	23872	1321	79719186
Cardiac ventricular scarring	19.26	17.84	3	23878	3	79720504
Anxiety	19.10	17.84	28	23853	248484	79472023
Pericarditis	19.01	17.84	4	23877	104232	79616275
Intentional product use issue	18.95	17.84	11	23870	152101	79568406
Haemoglobin urine present	18.94	17.84	8	23873	947	79719560
Tremor	18.88	17.84	14	23867	170069	79550438
Neoplasm	18.68	17.84	18	23863	9098	79711409
Blood bilirubin abnormal	18.63	17.84	9	23872	1456	79719051
Stomatitis	18.50	17.84	90	23791	146667	79573840
Wound	18.26	17.84	6	23875	116173	79604334
Peripheral swelling	18.26	17.84	33	23848	269584	79450923
Metastases to pelvis	18.15	17.84	7	23874	655	79719852

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EX03	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors
FDA MoA	N0000175076	Protein Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor
FDA MoA	N0000182137	Cytochrome P450 2D6 Inhibitors
FDA MoA	N0000182141	Cytochrome P450 3A4 Inhibitors
FDA MoA	N0000187062	Cytochrome P450 2C8 Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
CHEBI has role	CHEBI:65207	vascular endothelial growth factor receptor inhibitors

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

Disease	Relation	SNOMED_ID	DOID
Sarcoma of soft tissue	indication	424952003
Renal cell carcinoma	indication	702391001	DOID:4450
Hypocalcemia	contraindication	5291005
Acute hemorrhage	contraindication	8573003
Hyperbilirubinemia	contraindication	14783006	DOID:2741
Myocardial infarction	contraindication	22298006	DOID:5844
Proteinuria	contraindication	29738008	DOID:576
Torsades de pointes	contraindication	31722008
Gastrointestinal fistula	contraindication	37831005
Hypertensive disorder	contraindication	38341003	DOID:10763
Hypothyroidism	contraindication	40930008	DOID:1459
Hypokalemia	contraindication	43339004
Gastrointestinal perforation	contraindication	51875005
Hepatic failure	contraindication	59927004
Diarrhea	contraindication	62315008
Gastrointestinal hemorrhage	contraindication	74474003
Pancreatitis	contraindication	75694006	DOID:4989
Prolonged QT interval	contraindication	111975006
Liver function tests abnormal	contraindication	166603001
Hypomagnesemia	contraindication	190855004
Angina pectoris	contraindication	194828000
Drug-induced hepatitis	contraindication	235876009
Impaired wound healing	contraindication	271618001
Cerebral hemorrhage	contraindication	274100004
Pregnancy, function	contraindication	289908002
Thromboembolic disorder	contraindication	371039008
Surgical procedure	contraindication	387713003
Cardiovascular event risk	contraindication	395112001
UGT1A1*28 polymorphism	contraindication	430235005
Congenital long QT syndrome	contraindication	442917000
Hypertensive urgency	contraindication	443482000
Acute Thromboembolic Stroke	contraindication

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.3	acidic
pKa2	5.69	Basic
pKa3	1.23	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])	Bioact source	MoA source
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	Kd	7.85	CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN	INHIBITOR	Kd	7.57	CHEMBL	CHEMBL
Macrophage colony-stimulating factor 1 receptor	Kinase	P07333	CSF1R_HUMAN	INHIBITOR	Kd	8.10	CHEMBL	CHEMBL
Platelet-derived growth factor receptor alpha	Kinase	P16234	PGFRA_HUMAN	INHIBITOR	Kd	8.31	CHEMBL	CHEMBL
Tyrosine-protein kinase ITK/TSK	Kinase	Q08881	ITK_HUMAN	INHIBITOR			CHEMBL	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN	INHIBITOR	Kd	8.74	CHEMBL	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN	INHIBITOR	Kd	8.70	CHEMBL	CHEMBL
Fibroblast growth factor receptor 3	Kinase	P22607	FGFR3_HUMAN	INHIBITOR	Kd	6.21	CHEMBL	CHEMBL
Tyrosine-protein kinase Lck	Kinase	P06239	LCK_HUMAN	INHIBITOR	Kd	5.92	CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN	INHIBITOR	Kd	7.85	CHEMBL	CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN	INHIBITOR	Kd	6	CHEMBL	CHEMBL
Calcium/calmodulin-dependent protein kinase type 1	Kinase	Q14012	KCC1A_HUMAN		Kd	5.68	CHEMBL
Mitogen-activated protein kinase 8	Kinase	P45983	MK08_HUMAN		Kd	5.70	CHEMBL
Tyrosine-protein kinase HCK	Kinase	P08631	HCK_HUMAN		Kd	5.24	CHEMBL
Mitogen-activated protein kinase 10	Kinase	P53779	MK10_HUMAN		Kd	5.72	CHEMBL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN		Kd	5.77	CHEMBL
Tyrosine-protein kinase SYK	Kinase	P43405	KSYK_HUMAN		Kd	5.33	CHEMBL
Myosin light chain kinase 2, skeletal/cardiac muscle	Kinase	Q9H1R3	MYLK2_HUMAN		Kd	5.70	CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		Kd	5.48	CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN		Kd	5.54	CHEMBL
Hepatocyte growth factor receptor	Kinase	P08581	MET_HUMAN		Kd	5.70	CHEMBL
Tyrosine-protein kinase Lyn	Kinase	P07948	LYN_HUMAN		Kd	6.05	CHEMBL
Serine/threonine-protein kinase Nek2	Kinase	P51955	NEK2_HUMAN		Kd	6.01	CHEMBL
LIM domain kinase 1	Kinase	P53667	LIMK1_HUMAN		Kd	6.14	CHEMBL
Serine/threonine-protein kinase 10	Kinase	O94804	STK10_HUMAN		Kd	7.08	CHEMBL
Tyrosine-protein kinase Fer	Kinase	P16591	FER_HUMAN		Kd	5.57	CHEMBL
Serine/threonine-protein kinase PLK4	Kinase	O00444	PLK4_HUMAN		Kd	6.54	CHEMBL
Aurora kinase C	Kinase	Q9UQB9	AURKC_HUMAN		Kd	6.12	CHEMBL
Serine/threonine-protein kinase 16	Kinase	O75716	STK16_HUMAN		Kd	6.44	CHEMBL
Dual specificity protein kinase TTK	Kinase	P33981	TTK_HUMAN		Kd	6.82	CHEMBL
Abelson tyrosine-protein kinase 2	Kinase	P42684	ABL2_HUMAN		Kd	5.52	CHEMBL
Fibroblast growth factor receptor 2	Kinase	P21802	FGFR2_HUMAN		Kd	6.68	CHEMBL
TRAF2 and NCK-interacting protein kinase	Kinase	Q9UKE5	TNIK_HUMAN		Kd	6.51	CHEMBL
Tyrosine-protein kinase Fgr	Kinase	P09769	FGR_HUMAN		Kd	5.80	CHEMBL
Aurora kinase A	Kinase	O14965	AURKA_HUMAN		Kd	5.15	CHEMBL
ALK tyrosine kinase receptor	Kinase	Q9UM73	ALK_HUMAN		Kd	5.66	CHEMBL
Serine/threonine-protein kinase 36	Kinase	Q9NRP7	STK36_HUMAN		Kd	6.33	CHEMBL
BMP-2-inducible protein kinase	Kinase	Q9NSY1	BMP2K_HUMAN		Kd	5.06	CHEMBL
Tyrosine-protein kinase FRK	Kinase	P42685	FRK_HUMAN		Kd	6.12	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5	Kinase	Q9Y4K4	M4K5_HUMAN		Kd	5.52	CHEMBL
Cyclin-G-associated kinase	Kinase	O14976	GAK_HUMAN		Kd	6.70	CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	6.24	CHEMBL
Cyclin-dependent kinase 16	Kinase	Q00536	CDK16_HUMAN		Kd	5.92	CHEMBL
STE20-like serine/threonine-protein kinase	Kinase	Q9H2G2	SLK_HUMAN		Kd	6.62	CHEMBL
MAP/microtubule affinity-regulating kinase 3	Kinase	P27448	MARK3_HUMAN		Kd	5.40	CHEMBL
Calcium/calmodulin-dependent protein kinase type 1G	Kinase	Q96NX5	KCC1G_HUMAN		Kd	5.43	CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	7.24	CHEMBL
TGF-beta receptor type-2	Kinase	P37173	TGFR2_HUMAN		Kd	5.52	CHEMBL
Protein-tyrosine kinase 6	Kinase	Q13882	PTK6_HUMAN		Kd	5.64	CHEMBL
Non-receptor tyrosine-protein kinase TNK1	Kinase	Q13470	TNK1_HUMAN		Kd	6.01	CHEMBL
Non-receptor tyrosine-protein kinase TYK2	Kinase	P29597	TYK2_HUMAN		Kd	5.47	CHEMBL
Tyrosine-protein kinase receptor Tie-1	Kinase	P35590	TIE1_HUMAN		Kd	6.15	CHEMBL
Tyrosine-protein kinase TXK	Kinase	P42681	TXK_HUMAN		Kd	5.59	CHEMBL
LIM domain kinase 2	Kinase	P53671	LIMK2_HUMAN		Kd	6.41	CHEMBL
Serine/threonine-protein kinase NLK	Kinase	Q9UBE8	NLK_HUMAN		Kd	5.36	CHEMBL
Interleukin-1 receptor-associated kinase 3	Kinase	Q9Y616	IRAK3_HUMAN		Kd	6.10	CHEMBL
Serine/threonine-protein kinase SIK2	Kinase	Q9H0K1	SIK2_HUMAN		Kd	5.14	CHEMBL
Activin receptor type-2B	Kinase	Q13705	AVR2B_HUMAN		Kd	5.62	CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	7.01	CHEMBL
Leukocyte tyrosine kinase receptor	Kinase	P29376	LTK_HUMAN		Kd	5.17	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 1	Kinase	Q92918	M4K1_HUMAN		Kd	6.12	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 3	Kinase	Q8IVH8	M4K3_HUMAN		Kd	5.80	CHEMBL
Tyrosine-protein kinase Blk	Kinase	P51451	BLK_HUMAN		Kd	5.59	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4	Kinase	O95819	M4K4_HUMAN		Kd	5.66	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 4	Kinase	P45985	MP2K4_HUMAN		Kd	6.23	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 6	Kinase	P52564	MP2K6_HUMAN		Kd	5.39	CHEMBL
Tyrosine-protein kinase Mer	Kinase	Q12866	MERTK_HUMAN		Kd	5.48	CHEMBL
Cyclin-dependent kinase 11B	Kinase	P21127	CD11B_HUMAN		Kd	5.68	CHEMBL
Cyclin-dependent kinase 11A	Kinase	Q9UQ88	CD11A_HUMAN		Kd	5.89	CHEMBL
Mitogen-activated protein kinase kinase kinase 9	Kinase	P80192	M3K9_HUMAN		Kd	6.54	CHEMBL
Mitogen-activated protein kinase kinase kinase 10	Kinase	Q02779	M3K10_HUMAN		Kd	5.68	CHEMBL
Mitogen-activated protein kinase kinase kinase 11	Kinase	Q16584	M3K11_HUMAN		Kd	6.13	CHEMBL
Serine/threonine-protein kinase Nek5	Kinase	Q6P3R8	NEK5_HUMAN		Kd	5.14	CHEMBL
Serine/threonine-protein kinase SIK1	Kinase	P57059	SIK1_HUMAN		Kd	5.66	CHEMBL
Tyrosine-protein kinase Srms	Kinase	Q9H3Y6	SRMS_HUMAN		Kd	5.60	CHEMBL
Interferon-induced, double-stranded RNA-activated protein kinase	Kinase	P19525	E2AK2_HUMAN		Kd	5.72	CHEMBL
Receptor-interacting serine/threonine-protein kinase 1	Kinase	Q13546	RIPK1_HUMAN		Kd	6.59	CHEMBL
Tyrosine-protein kinase Fes/Fps	Kinase	P07332	FES_HUMAN		Kd	5.85	CHEMBL
Fibroblast growth factor receptor 4	Kinase	P22455	FGFR4_HUMAN		Kd	5.55	CHEMBL
Proto-oncogene tyrosine-protein kinase ROS	Kinase	P08922	ROS1_HUMAN		Kd	6.04	CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 2	Kinase	Q12851	M4K2_HUMAN		Kd	5.57	CHEMBL
Ephrin type-B receptor 6	Kinase	O15197	EPHB6_HUMAN		Kd	7.09	CHEMBL
Interleukin-1 receptor-associated kinase 1	Kinase	P51617	IRAK1_HUMAN		Kd	5.23	CHEMBL
Mitogen-activated protein kinase kinase kinase 2	Kinase	Q9Y2U5	M3K2_HUMAN		Kd	6.54	CHEMBL
Serine/threonine-protein kinase RIO2	Kinase	Q9BVS4	RIOK2_HUMAN		Kd	6.21	CHEMBL
Serine/threonine-protein kinase TAO1	Kinase	Q7L7X3	TAOK1_HUMAN		Kd	6.62	CHEMBL
Serine/threonine-protein kinase TAO3	Kinase	Q9H2K8	TAOK3_HUMAN		Kd	7.35	CHEMBL
Mitogen-activated protein kinase kinase kinase 19	Kinase	Q56UN5	M3K19_HUMAN		Kd	6.03	CHEMBL
Mitogen-activated protein kinase kinase kinase 1	Kinase	Q13233	M3K1_HUMAN		Kd	5.54	CHEMBL
Phosphatidylinositol 4-kinase beta	Kinase	Q9UBF8	PI4KB_HUMAN		Kd	6.02	CHEMBL
Bone morphogenetic protein receptor type-1B	Kinase	O00238	BMR1B_HUMAN		Kd	6	CHEMBL
Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma	Kinase	O60331	PI51C_HUMAN		Kd	5.72	CHEMBL
Serine/threonine-protein kinase TAO2	Kinase	Q9UL54	TAOK2_HUMAN		Kd	5.74	CHEMBL
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma	Kinase	Q8TBX8	PI42C_HUMAN		Kd	6.55	CHEMBL
Dual specificity mitogen-activated protein kinase kinase 5	Kinase	Q13163	MP2K5_HUMAN		Kd	6.32	CHEMBL
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN		Kd	5.73	CHEMBL
Tyrosine-protein kinase JAK3	Kinase	P52333	JAK3_HUMAN		Kd	5.16	CHEMBL
Uncharacterized aarF domain-containing protein kinase 1	Kinase	Q86TW2	ADCK1_HUMAN		Kd	4.79	CHEMBL
Acetylcholinesterase	Enzyme	P22303	ACES_HUMAN		IC50	6.03	CHEMBL
Carbonic anhydrase 9	Enzyme	Q16790	CAH9_HUMAN		Ki	8.04	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	6.42	CHEMBL
Proto-oncogene tyrosine-protein kinase Src	Kinase	P12931	SRC_HUMAN		Kd	5.55	CHEMBL
Tyrosine-protein kinase Yes	Kinase	P07947	YES_HUMAN		Kd	5.30	CHEMBL
Tyrosine-protein kinase Fyn	Kinase	P06241	FYN_HUMAN		Kd	5.57	CHEMBL
RAF proto-oncogene serine/threonine-protein kinase	Kinase	P04049	RAF1_HUMAN		Kd	6.05	CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN		Kd	6.37	CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		Kd	6.13	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	6.57	CHEMBL
Calcium-dependent protein kinase 1	Kinase		CDPK1_PLAF7		Kd	6.43	CHEMBL

External reference:

ID	Source
4029464	VUID
N0000180309	NUI
D05380	KEGG_DRUG
635702-64-6	SECONDARY_CAS_RN
4029464	VANDF
C1831796	UMLSCUI
CHEBI:71219	CHEBI
CHEMBL477772	ChEMBL_ID
CHEMBL1201733	ChEMBL_ID
DB06589	DRUGBANK_ID
C516667	MESH_SUPPLEMENTAL_RECORD_UI
5698	IUPHAR_LIGAND_ID
8681	INN_ID
7RN5DR86CK	UNII
10113978	PUBCHEM_CID
714438	RXNORM
168598	MMSL
26797	MMSL
d07499	MMSL
013302	NDDF
013303	NDDF
443763005	SNOMEDCT_US
443764004	SNOMEDCT_US
735169009	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
VOTRIENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0670	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections
VOTRIENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0670	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections
VOTRIENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-0670	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections
VOTRIENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1077	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections
VOTRIENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1077	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections
VOTRIENT	HUMAN PRESCRIPTION DRUG LABEL	1	0078-1077	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections