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

Stem definition	Drug id	CAS RN
Raf (Rapidely Accelerated Fibrosarcoma) kinase inhibitors	4654	755037-03-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: regorafenib monohydrate Stivarga regorafenib regorafenib hydrate anhydrous regorafenib BAY 73-4506	Regorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, metastasis and tumor immunity. In in vitro biochemical or cellular assays, regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAF V600E, SAPK2, PTK5, Abl and CSF1R at concentrations of regorafenib that have been achieved clinically. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model and inhibition of tumor growth in several mouse xenograft models including some for human colorectal carcinoma, gastrointestinal stromal and hepatocellular carcinoma. Regorafenib also demonstrated anti-metastatic activity in a mouse xenograft model and two mouse orthotopic models of human colorectal carcinoma. Molecular weight: 482.82 Formula: C21H15ClF4N4O3 CLOGP: 4.88 LIPINSKI: 1 HAC: 7 HDO: 3 TPSA: 92.35 ALOGS: -5.67 ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

regorafenib monohydrate
Stivarga
regorafenib
regorafenib hydrate
anhydrous regorafenib
BAY 73-4506

Regorafenib is a small molecule inhibitor of multiple membrane-bound and intracellular kinases involved in normal cellular functions and in pathologic processes such as oncogenesis, tumor angiogenesis, metastasis and tumor immunity. In in vitro biochemical or cellular assays, regorafenib or its major human active metabolites M-2 and M-5 inhibited the activity of RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, TrkA, Eph2A, RAF-1, BRAF, BRAF V600E, SAPK2, PTK5, Abl and CSF1R at concentrations of regorafenib that have been achieved clinically. In in vivo models, regorafenib demonstrated anti-angiogenic activity in a rat tumor model and inhibition of tumor growth in several mouse xenograft models including some for human colorectal carcinoma, gastrointestinal stromal and hepatocellular carcinoma. Regorafenib also demonstrated anti-metastatic activity in a mouse xenograft model and two mouse orthotopic models of human colorectal carcinoma.

Molecular weight: 482.82
Formula: C21H15ClF4N4O3
CLOGP: 4.88
LIPINSKI: 1
HAC: 7
HDO: 3
TPSA: 92.35
ALOGS: -5.67
ROTB: 6

Status: ONP

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

Drug dosage:

Dose	Unit	Route
0.12	g	O

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
Aug. 26, 2013	EMA
Sept. 27, 2012	FDA	BAYER HLTHCARE

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
Palmar-plantar erythrodysaesthesia syndrome	1291.47	25.89	375	12111	22640	63453896
Dysphonia	432.37	25.89	203	12283	47411	63429125
Decreased appetite	252.19	25.89	277	12209	250775	63225761
Off label use	240.22	25.89	453	12033	674009	62802527
Metastases to lung	182.59	25.89	75	12411	12675	63463861
Fatigue	156.59	25.89	453	12033	887575	62588961
Diarrhoea	119.94	25.89	359	12127	715007	62761529
Hyperkeratosis	112.74	25.89	43	12443	5975	63470561
Asthenia	109.64	25.89	236	12250	383368	63093168
Blood bilirubin increased	109.51	25.89	76	12410	37064	63439472
Carcinoembryonic antigen increased	108.64	25.89	31	12455	1734	63474802
Metastases to liver	108.61	25.89	64	12422	23575	63452961
Skin exfoliation	106.02	25.89	79	12407	43023	63433513
Pyrexia	105.45	25.89	263	12223	470215	63006321
Neuropathy peripheral	101.04	25.89	118	12368	113549	63362987
Pain in extremity	97.01	25.89	206	12280	331280	63145256
Hypertension	90.41	25.89	181	12305	279122	63197414
Blister	83.94	25.89	115	12371	129699	63346837
Platelet count decreased	81.38	25.89	107	12379	116015	63360521
Dehydration	79.81	25.89	131	12355	173223	63303313
Oral pain	78.79	25.89	56	12430	28338	63448198
Weight decreased	67.39	25.89	160	12326	276638	63199898
Stomatitis	66.76	25.89	107	12379	138618	63337918
Blood pressure increased	64.72	25.89	115	12371	161947	63314589
Rash	64.00	25.89	248	12238	560623	62915913
Hepatic function abnormal	61.42	25.89	54	12432	37088	63439448
Dry skin	60.68	25.89	65	12421	56822	63419714
Condition aggravated	57.84	25.89	6	12480	402211	63074325
Disseminated intravascular coagulation	51.52	25.89	37	12449	19014	63457522
Colon cancer	51.37	25.89	29	12457	9849	63466687
Drug ineffective	49.70	25.89	81	12405	1044684	62431852
Skin toxicity	48.61	25.89	22	12464	4692	63471844
Hospitalisation	48.47	25.89	71	12415	85010	63391526
Tumour marker increased	47.74	25.89	22	12464	4893	63471643
Erythema	45.32	25.89	104	12382	175647	63300889
Plantar erythema	44.21	25.89	10	12476	216	63476320
Mucosal inflammation	43.78	25.89	50	12436	46878	63429658
Colorectal cancer metastatic	43.33	25.89	12	12474	601	63475935
Skin fissures	42.48	25.89	27	12459	11361	63465175
Abdominal pain	40.28	25.89	138	12348	293318	63183218
Jaundice	39.54	25.89	38	12448	29213	63447323
Exercise tolerance decreased	39.45	25.89	20	12466	5477	63471059
Ascites	37.32	25.89	43	12443	40685	63435851
Aspartate aminotransferase increased	35.91	25.89	64	12422	90213	63386323
Gait inability	35.81	25.89	48	12438	52911	63423625
Hepatic encephalopathy	35.38	25.89	24	12462	11258	63465278
Joint swelling	34.11	25.89	11	12475	327655	63148881
Dry mouth	31.99	25.89	56	12430	77807	63398729
Colon cancer metastatic	31.95	25.89	11	12475	1140	63475396
Hepatic failure	31.59	25.89	37	12449	35619	63440917
Nasopharyngitis	31.36	25.89	6	12480	254251	63222285
Feeding disorder	29.54	25.89	23	12463	13339	63463197
Constipation	29.28	25.89	104	12382	224839	63251697
Intestinal obstruction	28.94	25.89	33	12453	30866	63445670
Myelosuppression	28.70	25.89	29	12457	23674	63452862
Drug hypersensitivity	28.08	25.89	13	12473	310674	63165862
Rash maculo-papular	26.44	25.89	32	12454	31864	63444672
Metastases to peritoneum	26.10	25.89	13	12473	3429	63473107

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
Palmar-plantar erythrodysaesthesia syndrome	2024.10	22.56	599	15527	16196	34924609
Dysphonia	707.69	22.56	299	15827	23084	34917721
Metastases to lung	356.01	22.56	141	15985	9179	34931626
Decreased appetite	335.36	22.56	397	15729	165995	34774810
Off label use	307.12	22.56	625	15501	418899	34521906
Fatigue	275.30	22.56	556	15570	370097	34570708
Metastases to liver	222.72	22.56	114	16012	13549	34927256
Diarrhoea	209.09	22.56	514	15612	389398	34551407
Blister	200.02	22.56	127	15999	22731	34918074
Hypertension	165.85	22.56	255	15871	136188	34804617
Carcinoembryonic antigen increased	152.86	22.56	40	16086	665	34940140
Pain in extremity	129.78	22.56	219	15907	126294	34814511
Blood bilirubin increased	122.16	22.56	117	16009	38179	34902626
Skin exfoliation	117.54	22.56	99	16027	27333	34913472
Asthenia	113.78	22.56	307	15819	244944	34695861
Skin fissures	97.77	22.56	48	16078	5211	34935594
Alpha 1 foetoprotein increased	97.02	22.56	28	16098	679	34940126
Neuropathy peripheral	95.90	22.56	152	15974	83111	34857694
Dry skin	91.18	22.56	91	16035	31196	34909609
Weight decreased	89.03	22.56	228	15898	176073	34764732
Stomatitis	87.66	22.56	103	16023	42411	34898394
Hyperkeratosis	87.42	22.56	40	16086	3709	34937096
Tumour marker increased	81.17	22.56	24	16102	635	34940170
Ascites	70.88	22.56	97	16029	46474	34894331
Hepatic function abnormal	68.42	22.56	93	16033	44270	34896535
Blood pressure increased	67.98	22.56	135	15991	87967	34852838
Metastases to lymph nodes	67.15	22.56	36	16090	4692	34936113
Hepatic encephalopathy	62.87	22.56	53	16073	14632	34926173
Hospitalisation	58.83	22.56	99	16027	56803	34884002
Oral pain	56.78	22.56	44	16082	10783	34930022
Toxicity to various agents	52.20	22.56	14	16112	200348	34740457
Colorectal cancer metastatic	49.79	22.56	17	16109	723	34940082
Dehydration	49.62	22.56	152	15974	129817	34810988
Aphonia	48.79	22.56	26	16100	3347	34937458
Gastrointestinal stromal tumour	48.71	22.56	18	16108	966	34939839
Abdominal pain upper	48.58	22.56	104	16022	71386	34869419
Abdominal pain	44.61	22.56	171	15955	163447	34777358
Glossodynia	43.87	22.56	25	16101	3668	34937137
Drug interaction	43.73	22.56	25	16101	225921	34714884
Colon cancer	42.96	22.56	34	16092	8587	34932218
Febrile neutropenia	40.83	22.56	7	16119	136842	34803963
Metastases to peritoneum	37.80	22.56	18	16108	1826	34938979
Condition aggravated	37.56	22.56	21	16105	192175	34748630
Colon cancer metastatic	36.60	22.56	17	16109	1630	34939175
Drug ineffective	35.08	22.56	102	16024	456649	34484156
Malaise	33.73	22.56	172	15954	185653	34755152
Acute kidney injury	33.33	22.56	56	16070	304932	34635873
Jaundice	32.30	22.56	55	16071	31827	34908978
Proteinuria	31.67	22.56	41	16085	18601	34922204
Hepatic failure	31.65	22.56	57	16069	34474	34906331
Metastasis	31.25	22.56	21	16105	4123	34936682
Biliary obstruction	31.05	22.56	18	16108	2727	34938078
Metastases to adrenals	30.72	22.56	13	16113	999	34939806
Metastases to central nervous system	29.85	22.56	27	16099	8178	34932627
Dry mouth	29.20	22.56	51	16075	30114	34910691
Angular cheilitis	28.67	22.56	8	16118	171	34940634
Overdose	28.65	22.56	4	16122	91055	34849750
Cardiac arrest	28.49	22.56	5	16121	96154	34844651
Gait inability	28.23	22.56	41	16085	20717	34920088
Constipation	27.84	22.56	131	15995	136851	34803954
Hypotension	27.77	22.56	37	16089	221612	34719193
Myelosuppression	26.13	22.56	38	16088	19227	34921578
Protein induced by vitamin K absence or antagonist II increased	25.79	22.56	5	16121	18	34940787
Ammonia increased	25.65	22.56	19	16107	4350	34936455
General physical health deterioration	25.57	22.56	122	16004	128147	34812658
Plantar erythema	24.44	22.56	6	16120	76	34940729
Hepatic pain	23.18	22.56	12	16114	1456	34939349
Gait disturbance	23.16	22.56	89	16037	85051	34855754
Rectal cancer metastatic	22.96	22.56	7	16119	206	34940599
Nephrotic syndrome	22.66	22.56	22	16104	7281	34933524

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
Palmar-plantar erythrodysaesthesia syndrome	3002.37	22.15	885	26232	32249	79685022
Dysphonia	1043.08	22.15	467	26650	56405	79660866
Decreased appetite	538.02	22.15	620	26497	341798	79375473
Metastases to lung	533.95	22.15	209	26908	17954	79699317
Off label use	487.54	22.15	995	26122	906220	78811051
Fatigue	361.98	22.15	898	26219	928829	78788442
Diarrhoea	308.59	22.15	818	26299	879671	78837600
Metastases to liver	305.37	22.15	162	26955	28152	79689119
Asthenia	233.32	22.15	527	26590	511162	79206109
Neuropathy peripheral	224.49	22.15	258	26859	141047	79576224
Blood bilirubin increased	217.10	22.15	180	26937	66052	79651219
Hypertension	212.42	22.15	393	26724	330599	79386672
Skin exfoliation	210.91	22.15	164	26953	54936	79662335
Carcinoembryonic antigen increased	208.04	22.15	61	27056	2148	79715123
Blister	199.66	22.15	224	26893	119252	79598019
Pain in extremity	197.53	22.15	403	26714	364135	79353136
Hyperkeratosis	161.94	22.15	70	27047	7720	79709551
Weight decreased	146.28	22.15	352	26765	354846	79362425
Dry skin	140.94	22.15	143	26974	67852	79649419
Skin fissures	138.64	22.15	74	27043	12999	79704272
Stomatitis	129.36	22.15	201	26916	146556	79570715
Hepatic function abnormal	125.35	22.15	139	26978	72968	79644303
Oral pain	122.39	22.15	95	27022	31703	79685568
Dehydration	119.78	22.15	262	26855	247925	79469346
Blood pressure increased	116.96	22.15	236	26881	211124	79506147
Alpha 1 foetoprotein increased	106.41	22.15	29	27088	779	79716492
Colon cancer	99.86	22.15	62	27055	14461	79702810
Condition aggravated	95.91	22.15	26	27091	501098	79216173
Ascites	93.91	22.15	122	26995	75440	79641831
Pyrexia	93.27	22.15	466	26651	678243	79039028
Hospitalisation	92.84	22.15	136	26981	94100	79623171
Tumour marker increased	90.79	22.15	39	27078	4233	79713038
Platelet count decreased	84.36	22.15	197	26920	194467	79522804
Colon cancer metastatic	78.08	22.15	29	27088	2152	79715119
Toxicity to various agents	76.72	22.15	24	27093	421516	79295755
Abdominal pain	74.14	22.15	295	26822	389274	79327997
Colorectal cancer metastatic	73.47	22.15	24	27093	1214	79716057
Hepatic encephalopathy	71.56	22.15	62	27055	24104	79693167
Drug ineffective	68.77	22.15	168	26949	1080745	78636526
Metastases to lymph nodes	65.51	22.15	42	27075	10355	79706916
Jaundice	64.50	22.15	85	27032	53264	79664007
Rash	61.06	22.15	370	26747	577988	79139283
Drug interaction	60.43	22.15	33	27084	415150	79302121
Metastases to peritoneum	58.65	22.15	29	27088	4343	79712928
Hepatic failure	56.90	22.15	86	27031	61126	79656145
Gait inability	56.51	22.15	84	27033	58833	79658438
Mucosal inflammation	56.30	22.15	96	27021	75484	79641787
Plantar erythema	54.11	22.15	14	27103	306	79716965
Abdominal pain upper	53.87	22.15	183	26934	223636	79493635
Infusion related reaction	52.14	22.15	8	27109	230229	79487042
Myelosuppression	51.51	22.15	66	27051	40230	79677041
Proteinuria	50.91	22.15	59	27058	32443	79684828
Gastrointestinal stromal tumour	50.75	22.15	20	27097	1743	79715528
Dry mouth	50.65	22.15	100	27017	87919	79629352
Aspartate aminotransferase increased	49.13	22.15	130	26987	138511	79578760
Constipation	48.76	22.15	208	26909	282842	79434429
Drug hypersensitivity	47.65	22.15	21	27096	298895	79418376
Exercise tolerance decreased	45.96	22.15	32	27085	9039	79708232
Death	45.63	22.15	339	26778	566175	79151096
Erythema	45.57	22.15	173	26944	223117	79494154
Weight increased	44.99	22.15	19	27098	277367	79439904
Disseminated intravascular coagulation	44.71	22.15	58	27059	35784	79681487
Sinusitis	43.79	22.15	7	27110	195494	79521777
Arthropathy	42.84	22.15	5	27112	177106	79540165
Overdose	42.63	22.15	6	27111	184200	79533071
Metastases to adrenals	41.51	22.15	16	27101	1314	79715957
Joint swelling	40.45	22.15	24	27093	288622	79428649
Biliary obstruction	40.06	22.15	23	27094	4651	79712620
Pain of skin	38.31	22.15	35	27082	14578	79702693
Skin toxicity	36.77	22.15	27	27090	8287	79708984
Acute kidney injury	36.72	22.15	76	27041	519328	79197943
Cardiac arrest	36.71	22.15	7	27110	172089	79545182
Metastasis	36.57	22.15	25	27092	6855	79710416
Ammonia increased	36.51	22.15	26	27091	7609	79709662
Pre-existing condition improved	36.35	22.15	23	27094	5540	79711731
Nasopharyngitis	35.72	22.15	21	27096	253860	79463411
Feeding disorder	35.14	22.15	35	27082	16219	79701052
Gastrointestinal perforation	34.29	22.15	23	27094	6114	79711157
Treatment failure	34.18	22.15	8	27109	170478	79546793
Fall	33.09	22.15	73	27044	487556	79229715
Therapeutic product ineffective	32.66	22.15	15	27102	1907	79715364
Protein induced by vitamin K absence or antagonist II increased	32.48	22.15	6	27111	23	79717248
Rectal cancer	32.03	22.15	18	27099	3495	79713776
Aphonia	31.63	22.15	27	27090	10285	79706986
Hypotension	31.47	22.15	64	27053	440253	79277018
Hypersomnia	31.39	22.15	39	27078	23047	79694224
Decreased activity	31.34	22.15	25	27092	8669	79708602
Gait disturbance	30.83	22.15	146	26971	207360	79509911
Asthma	29.88	22.15	5	27112	135090	79582181
Food refusal	29.80	22.15	10	27107	550	79716721
Hyperbilirubinaemia	29.53	22.15	39	27078	24479	79692792
Musculoskeletal stiffness	28.34	22.15	12	27105	174996	79542275
Oral hyperaesthesia	27.95	22.15	4	27113	0	79717271
Intestinal obstruction	27.34	22.15	51	27066	42969	79674302
Tumour rupture	27.27	22.15	9	27108	470	79716801
Anxiety	26.76	22.15	27	27090	248485	79468786
Febrile neutropenia	26.15	22.15	24	27093	230975	79486296
Protein urine present	26.08	22.15	24	27093	10088	79707183
Pancytopenia	25.84	22.15	12	27105	165733	79551538
Abnormal loss of weight	25.83	22.15	22	27095	8354	79708917
Liver disorder	25.73	22.15	68	27049	72349	79644922
Cancer pain	25.40	22.15	18	27099	5227	79712044
Skin induration	25.38	22.15	17	27100	4508	79712763
Arthralgia	24.89	22.15	105	27012	571698	79145573
Disease progression	24.72	22.15	126	26991	184236	79533035
Hepatic pain	24.54	22.15	16	27101	4056	79713215
Metastases to central nervous system	24.43	22.15	29	27088	16346	79700925
Metastases to abdominal cavity	24.40	22.15	9	27108	655	79716616
Depression	23.98	22.15	23	27094	216767	79500504
Chromaturia	23.67	22.15	36	27081	25710	79691561
Pneumonia	23.65	22.15	130	26987	660116	79057155
Syncope	23.64	22.15	16	27101	179433	79537838
Hepatic lesion	22.95	22.15	19	27098	6940	79710331
Osteosarcoma metastatic	22.87	22.15	5	27112	51	79717220
Skin disorder	22.53	22.15	41	27076	33902	79683369
Wheezing	22.36	22.15	6	27111	116658	79600613
Adverse drug reaction	22.24	22.15	61	27056	66331	79650940

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01EX05	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	N0000185504	Cytochrome P450 2C9 Inhibitors
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:38637	tyrosine kinase inhibitors
CHEBI has role	CHEBI:50908	agente hepatotoxico

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

Disease	Relation	SNOMED_ID	DOID
Liver cell carcinoma	indication	109841003	DOID:684
Metastasis from malignant tumor of colon	indication	314998002
Gastrointestinal stromal tumor	indication	420120006	DOID:9253

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.41	acidic
pKa2	11.83	acidic
pKa3	12.52	acidic
pKa4	2.76	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
40MG	STIVARGA	BAYER HLTHCARE	N203085	Sept. 27, 2012	RX	TABLET	ORAL	8680124	June 2, 2030	TREATMENT OF PATIENTS WITH GASTROINTESTINAL STROMAL TUMOR (GIST), INCLUDING BUT NOT LIMITED TO PATIENTS PREVIOUSLY TREATED WITH IMATINIB AND PATIENTS WITH GIST HAVING RESISTANCE TO A KIT TYROSINE KINASE INHIBITOR

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
40MG	STIVARGA	BAYER HLTHCARE	N203085	Sept. 27, 2012	RX	TABLET	ORAL	April 27, 2024	TREATMENT OF PATIENTS WITH HEPATOCELLULAR CARCINOMA (HCC OR LIVER CANCER) WHO HAVE BEEN PREVIOUSLY TREATED WITH THE DRUG SORAFENIB.

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	IC50	7.90	IUPHAR	CHEMBL
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN	INHIBITOR	IC50	7.55	CHEMBL	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		IC50	8.82	CHEMBL
Tyrosine-protein kinase ABL1	Kinase	P00519	ABL1_HUMAN		Kd	6.12	CHEMBL
Mast/stem cell growth factor receptor Kit	Kinase	P10721	KIT_HUMAN		IC50	8.21	CHEMBL
Breakpoint cluster region protein	Kinase	P11274	BCR_HUMAN		Kd	6.13	CHEMBL
Ephrin type-A receptor 2	Kinase	P29317	EPHA2_HUMAN		Kd	6.08	CHEMBL
RAF proto-oncogene serine/threonine-protein kinase	Kinase	P04049	RAF1_HUMAN		IC50	8.82	CHEMBL
Receptor-type tyrosine-protein kinase FLT3	Kinase	P36888	FLT3_HUMAN		IC50	7.09	CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret	Kinase	P07949	RET_HUMAN		Kd	6.90	CHEMBL
Vascular endothelial growth factor receptor 1	Kinase	P17948	VGFR1_HUMAN		IC50	8.82	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase	P35916	VGFR3_HUMAN		IC50	7.34	CHEMBL
Angiopoietin-1 receptor	Kinase	Q02763	TIE2_HUMAN		IC50	8.82	CHEMBL
LIM domain kinase 1	Kinase	P53667	LIMK1_HUMAN		Kd	6.21	CHEMBL
Fibroblast growth factor receptor 1	Kinase	P11362	FGFR1_HUMAN		IC50	8.82	CHEMBL
Dual specificity protein kinase TTK	Kinase	P33981	TTK_HUMAN		Kd	5.41	CHEMBL
Mitogen-activated protein kinase 11	Kinase	Q15759	MK11_HUMAN		Kd	5.72	CHEMBL
Ephrin type-A receptor 5	Kinase	P54756	EPHA5_HUMAN		Kd	5.95	CHEMBL
Mitogen-activated protein kinase 14	Kinase	Q16539	MK14_HUMAN		Kd	6.15	CHEMBL
Dual specificity protein kinase CLK1	Kinase	P49759	CLK1_HUMAN		Kd	5.68	CHEMBL
Receptor-interacting serine/threonine-protein kinase 2	Kinase	O43353	RIPK2_HUMAN		Kd	6.12	CHEMBL
Epithelial discoidin domain-containing receptor 1	Kinase	Q08345	DDR1_HUMAN		Kd	6.45	CHEMBL
Bifunctional epoxide hydrolase 2	Enzyme	P34913	HYES_HUMAN	INHIBITOR	IC50	9.30	CHEMBL
MAP kinase-activated protein kinase 2	Kinase	P49137	MAPK2_HUMAN		Kd	6.17	CHEMBL
Cyclin-dependent kinase 17	Kinase	Q00537	CDK17_HUMAN		Kd	6.14	CHEMBL
Mitogen-activated protein kinase kinase kinase MLT	Kinase	Q9NYL2	MLTK_HUMAN		Kd	6.56	CHEMBL
Discoidin domain-containing receptor 2	Kinase	Q16832	DDR2_HUMAN		Kd	6.38	CHEMBL
Ephrin type-A receptor 1	Kinase	P21709	EPHA1_HUMAN		Kd	8.15	CHEMBL
Mitogen-activated protein kinase kinase kinase 1	Kinase	Q13233	M3K1_HUMAN		Kd	6.33	CHEMBL
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	5.52	CHEMBL
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN		Kd	6.43	CHEMBL
Glycine receptor subunit alpha-1	Ion channel	P23415	GLRA1_HUMAN		EC50	5.74	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase		VGFR2_MOUSE		IC50	8.82	CHEMBL
Vascular endothelial growth factor receptor 3	Kinase		VGFR3_MOUSE		IC50	8.82	CHEMBL

External reference:

ID	Source
D10137	KEGG_DRUG
1019206-88-2	SECONDARY_CAS_RN
4031721	VANDF
CHEBI:68647	CHEBI
CHEMBL1946170	ChEMBL_ID
C559147	MESH_SUPPLEMENTAL_RECORD_UI
5891	IUPHAR_LIGAND_ID
DB08896	DRUGBANK_ID
MGN125FS9D	UNII
1312397	RXNORM
193440	MMSL
28887	MMSL
d07913	MMSL
014656	NDDF
702804006	SNOMEDCT_US
703808002	SNOMEDCT_US
C2980094	UMLSCUI
11167602	PUBCHEM_CID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Stivarga	HUMAN PRESCRIPTION DRUG LABEL	1	50419-171	TABLET, FILM COATED	40 mg	ORAL	NDA	29 sections
Stivarga	HUMAN PRESCRIPTION DRUG LABEL	1	50419-171	TABLET, FILM COATED	40 mg	ORAL	NDA	29 sections