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	1133.27	26.32	340	11216	19758	50573810
Dysphonia	417.76	26.32	195	11361	38697	50554871
Decreased appetite	245.93	26.32	264	11292	200659	50392909
Off label use	241.26	26.32	405	11151	474021	50119547
Metastases to lung	158.87	26.32	68	11488	10952	50582616
Fatigue	153.64	26.32	428	11128	707173	49886395
Blister	107.16	26.32	114	11442	85304	50508264
Hyperkeratosis	106.75	26.32	41	11515	4994	50588574
Skin exfoliation	106.12	26.32	76	11480	33536	50560032
Asthenia	102.58	26.32	225	11331	318817	50274751
Diarrhoea	101.63	26.32	329	11227	588147	50005421
Pyrexia	98.13	26.32	246	11310	379957	50213611
Metastases to liver	96.37	26.32	59	11497	20045	50573523
Carcinoembryonic antigen increased	96.16	26.32	28	11528	1446	50592122
Hypertension	91.78	26.32	169	11387	211034	50382534
Blood bilirubin increased	91.08	26.32	68	11488	31970	50561598
Pain in extremity	90.55	26.32	195	11361	272670	50320898
Neuropathy peripheral	89.00	26.32	110	11446	96647	50496921
Stomatitis	75.71	26.32	104	11452	101240	50492328
Oral pain	75.34	26.32	55	11501	24978	50568590
Dehydration	73.85	26.32	128	11428	152321	50441247
Weight decreased	70.89	26.32	156	11400	221089	50372479
Dry skin	65.68	26.32	64	11492	43127	50550441
Rash	65.00	26.32	233	11323	437238	50156330
Blood pressure increased	64.74	26.32	112	11444	133020	50460548
Platelet count decreased	62.97	26.32	95	11461	100631	50492937
Hepatic function abnormal	54.56	26.32	51	11505	32630	50560938
Hospitalisation	51.12	26.32	70	11486	67867	50525701
Drug ineffective	50.90	26.32	68	11488	819265	49774303
Disseminated intravascular coagulation	50.09	26.32	37	11519	17098	50576470
Condition aggravated	47.45	26.32	6	11550	297052	50296516
Skin fissures	45.56	26.32	27	11529	8641	50584927
Erythema	45.41	26.32	102	11454	146312	50447256
Mucosal inflammation	44.06	26.32	50	11506	40092	50553476
Skin toxicity	43.08	26.32	20	11536	3893	50589675
Plantar erythema	42.86	26.32	10	11546	213	50593355
Abdominal pain	42.15	26.32	134	11422	236094	50357474
Gait inability	42.14	26.32	47	11509	36980	50556588
Tumour marker increased	40.33	26.32	19	11537	3821	50589747
Dry mouth	39.44	26.32	56	11500	56122	50537446
Colorectal cancer metastatic	39.04	26.32	11	11545	504	50593064
Exercise tolerance decreased	38.90	26.32	20	11536	4854	50588714
Palmoplantar keratoderma	37.92	26.32	8	11548	105	50593463
Hepatic encephalopathy	35.57	26.32	24	11532	9612	50583956
Colon cancer	35.36	26.32	23	11533	8668	50584900
Jaundice	30.85	26.32	34	11522	26395	50567173
Constipation	29.20	26.32	101	11455	185607	50407961
Feeding disorder	28.97	26.32	22	11534	10591	50582977
Drug hypersensitivity	28.26	26.32	11	11545	250999	50342569
Joint swelling	27.20	26.32	11	11545	245275	50348293
Ascites	27.03	26.32	37	11519	35824	50557744
Hepatic failure	26.92	26.32	35	11521	32248	50561320

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	1889.48	23.25	564	14492	14195	29545276
Dysphonia	719.25	23.25	294	14762	18902	29540569
Decreased appetite	335.60	23.25	390	14666	144952	29414519
Metastases to lung	309.77	23.25	125	14931	7730	29551741
Off label use	300.03	23.25	541	14515	300259	29259212
Fatigue	273.74	23.25	536	14520	316285	29243186
Diarrhoea	201.22	23.25	488	14568	332210	29227261
Blister	199.63	23.25	125	14931	19781	29539690
Metastases to liver	175.90	23.25	96	14960	11760	29547711
Hypertension	155.72	23.25	240	14816	116374	29443097
Carcinoembryonic antigen increased	153.80	23.25	40	15016	584	29558887
Pain in extremity	134.53	23.25	218	14838	110215	29449256
Skin exfoliation	121.37	23.25	97	14959	22548	29536923
Blood bilirubin increased	118.81	23.25	114	14942	33779	29525692
Asthenia	106.88	23.25	294	14762	214956	29344515
Skin fissures	100.41	23.25	46	15010	3873	29555598
Neuropathy peripheral	98.57	23.25	149	14907	70878	29488593
Dry skin	96.39	23.25	86	14970	23221	29536250
Weight decreased	92.18	23.25	223	14833	150682	29408789
Stomatitis	85.75	23.25	100	14956	37013	29522458
Hyperkeratosis	85.73	23.25	39	15017	3230	29556241
Alpha 1 foetoprotein increased	84.20	23.25	25	15031	606	29558865
Tumour marker increased	78.94	23.25	23	15033	521	29558950
Ascites	76.91	23.25	94	14962	36525	29522946
Blood pressure increased	71.73	23.25	132	14924	73671	29485800
Hospitalisation	64.48	23.25	97	14959	45891	29513580
Hepatic function abnormal	64.08	23.25	89	14967	39170	29520301
Oral pain	58.85	23.25	44	15012	9263	29550208
Hepatic encephalopathy	57.68	23.25	50	15006	12985	29546486
Dehydration	52.06	23.25	152	14904	114596	29444875
Toxicity to various agents	50.68	23.25	13	15043	173648	29385823
Abdominal pain	48.29	23.25	165	14891	135192	29424279
Abdominal pain upper	48.16	23.25	100	14956	60893	29498578
Metastases to lymph nodes	47.34	23.25	28	15028	3989	29555482
Glossodynia	44.61	23.25	25	15031	3218	29556253
Aphonia	44.15	23.25	24	15032	2910	29556561
Drug interaction	40.90	23.25	25	15031	197360	29362111
Colorectal cancer metastatic	40.78	23.25	14	15042	547	29558924
Metastases to peritoneum	39.43	23.25	18	15038	1502	29557969
Dry mouth	37.96	23.25	51	15005	21733	29537738
Febrile neutropenia	37.71	23.25	6	15050	112234	29447237
Gastrointestinal stromal tumour	36.28	23.25	14	15042	766	29558705
Malaise	36.28	23.25	169	14887	159433	29400038
Drug ineffective	34.17	23.25	85	14971	363085	29196386
Colon cancer	33.12	23.25	29	15027	7626	29551845
Acute kidney injury	32.70	23.25	53	15003	265214	29294257
Condition aggravated	32.47	23.25	17	15039	146278	29413193
Constipation	30.56	23.25	127	14929	114033	29445438
Colon cancer metastatic	30.52	23.25	15	15041	1476	29557995
Proteinuria	29.07	23.25	38	15018	15766	29543705
Biliary obstruction	28.90	23.25	17	15039	2397	29557074
Hypotension	28.77	23.25	34	15022	194320	29365151
Angular cheilitis	28.49	23.25	8	15048	158	29559313
Cardiac arrest	27.80	23.25	5	15051	85586	29473885
Overdose	27.41	23.25	4	15052	79815	29479656
Colorectal cancer	27.34	23.25	15	15041	1852	29557619
Plantar erythema	26.34	23.25	6	15050	48	29559423
Gait inability	26.06	23.25	39	15017	18336	29541135
Protein induced by vitamin K absence or antagonist II increased	25.30	23.25	5	15051	18	29559453
Metastases to central nervous system	24.97	23.25	24	15032	7107	29552364
General physical health deterioration	24.88	23.25	111	14945	102746	29456725
Metastases to adrenals	24.25	23.25	11	15045	904	29558567
Adverse drug reaction	23.33	23.25	43	15013	23977	29535494

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	2704.01	21.41	817	24495	28002	64445418
Dysphonia	1038.01	21.41	457	24855	45925	64427495
Decreased appetite	532.64	21.41	601	24711	280688	64192732
Metastases to lung	470.01	21.41	189	25123	15075	64458345
Off label use	454.01	21.41	852	24460	631954	63841466
Fatigue	366.06	21.41	862	24450	747868	63725552
Diarrhoea	284.37	21.41	767	24545	721937	63751483
Metastases to liver	253.36	21.41	142	25170	23799	64449621
Blister	240.11	21.41	221	25091	80746	64392674
Asthenia	222.22	21.41	506	24806	427538	64045882
Neuropathy peripheral	214.41	21.41	247	25065	117278	64356142
Skin exfoliation	211.05	21.41	160	25152	44725	64428695
Hypertension	210.86	21.41	370	24942	258891	64214529
Carcinoembryonic antigen increased	200.54	21.41	59	25253	1814	64471606
Pain in extremity	198.35	21.41	394	24918	302691	64170729
Blood bilirubin increased	194.13	21.41	169	25143	57384	64416036
Hyperkeratosis	156.09	21.41	68	25244	6613	64466807
Weight decreased	154.81	21.41	344	24968	285395	64188025
Dry skin	150.30	21.41	139	25173	51022	64422398
Stomatitis	143.21	21.41	195	25117	109410	64364010
Skin fissures	142.34	21.41	73	25239	10233	64463187
Oral pain	122.58	21.41	95	25217	27398	64446022
Blood pressure increased	119.47	21.41	230	25082	172322	64301098
Dehydration	116.16	21.41	260	25052	216503	64256917
Hepatic function abnormal	113.51	21.41	133	25179	64180	64409240
Hospitalisation	99.99	21.41	135	25177	75072	64398348
Pyrexia	86.73	21.41	440	24872	558204	63915216
Alpha 1 foetoprotein increased	86.69	21.41	25	25287	715	64472705
Ascites	85.01	21.41	113	25199	61888	64411532
Toxicity to various agents	83.66	21.41	20	25292	363493	64109927
Tumour marker increased	83.48	21.41	36	25276	3414	64470006
Condition aggravated	82.80	21.41	22	25290	372404	64101016
Abdominal pain	80.26	21.41	287	25025	312088	64161332
Drug ineffective	77.68	21.41	132	25180	840115	63633305
Colon cancer	72.49	21.41	51	25261	12688	64460732
Dry mouth	67.75	21.41	100	25212	60318	64413102
Hepatic encephalopathy	67.24	21.41	60	25252	21006	64452414
Gait inability	65.56	21.41	82	25230	42286	64431134
Drug interaction	61.15	21.41	33	25279	362050	64111370
Abdominal pain upper	60.42	21.41	178	25134	174852	64298568
Colorectal cancer metastatic	59.82	21.41	20	25292	940	64472480
Rash	59.38	21.41	344	24968	458205	64015215
Platelet count decreased	59.27	21.41	172	25140	167539	64305881
Metastases to peritoneum	57.45	21.41	28	25284	3519	64469901
Mucosal inflammation	56.82	21.41	94	25218	62490	64410930
Colon cancer metastatic	56.36	21.41	23	25289	1900	64471520
Constipation	54.85	21.41	206	25106	229131	64244289
Plantar erythema	53.25	21.41	14	25298	281	64473139
Metastases to lymph nodes	49.83	21.41	35	25277	8682	64464738
Jaundice	46.93	21.41	75	25237	48437	64424983
Exercise tolerance decreased	46.52	21.41	32	25280	7678	64465742
Drug hypersensitivity	45.82	21.41	18	25294	237797	64235623
Erythema	44.67	21.41	168	25144	186902	64286518
Disseminated intravascular coagulation	42.85	21.41	58	25254	32290	64441130
Overdose	42.61	21.41	6	25306	159560	64313860
Hepatic failure	42.18	21.41	77	25235	55317	64418103
Infusion related reaction	42.06	21.41	7	25305	164460	64308960
Proteinuria	41.84	21.41	53	25259	27670	64445750
Acute kidney injury	40.04	21.41	72	25240	449168	64024252
Aspartate aminotransferase increased	39.57	21.41	120	25192	119668	64353752
Cardiac arrest	38.43	21.41	7	25305	154057	64319363
Gastrointestinal stromal tumour	38.38	21.41	16	25296	1395	64472025
Biliary obstruction	38.37	21.41	22	25290	3842	64469578
Hypotension	36.76	21.41	58	25254	380916	64092504
Weight increased	36.63	21.41	19	25293	213329	64260091
Skin toxicity	36.56	21.41	26	25286	6576	64466844
Colorectal cancer	36.50	21.41	20	25292	3201	64470219
Feeding disorder	35.72	21.41	34	25278	12915	64460505
Sinusitis	35.61	21.41	7	25305	145921	64327499
Palmoplantar keratoderma	35.22	21.41	11	25301	415	64473005
Febrile neutropenia	34.85	21.41	15	25297	187642	64285778
Fall	34.34	21.41	70	25242	416756	64056664
Pre-existing condition improved	34.12	21.41	22	25290	4740	64468680
Metastases to adrenals	34.09	21.41	14	25298	1175	64472245
Gastrointestinal perforation	33.88	21.41	23	25289	5401	64468019
Rectal cancer	33.40	21.41	18	25294	2788	64470632
Ammonia increased	33.04	21.41	25	25287	6952	64466468
Decreased activity	32.40	21.41	25	25287	7155	64466265
Protein induced by vitamin K absence or antagonist II increased	32.27	21.41	6	25306	20	64473400
Pain of skin	32.08	21.41	28	25284	9519	64463901
Arthropathy	31.26	21.41	5	25307	120962	64352458
Therapeutic product ineffective	30.84	21.41	14	25298	1499	64471921
Adverse drug reaction	30.65	21.41	60	25252	45404	64428016
Food refusal	30.44	21.41	10	25302	445	64472975
Joint swelling	30.38	21.41	24	25288	215358	64258062
Hypersomnia	30.23	21.41	38	25274	19679	64453741
Nasopharyngitis	30.06	21.41	20	25292	196053	64277367
Gait disturbance	29.67	21.41	140	25172	172015	64301405
Death	28.54	21.41	302	25010	482403	63991017
Aphonia	28.20	21.41	25	25287	8672	64464748
Oral hyperaesthesia	27.37	21.41	4	25308	0	64473420
Pancytopenia	27.33	21.41	11	25301	143298	64330122
Intestinal obstruction	27.06	21.41	50	25262	36236	64437184
Hyperbilirubinaemia	26.54	21.41	37	25275	21168	64452252
Liver disorder	26.28	21.41	62	25250	53289	64420131
Metastasis	26.07	21.41	20	25292	5675	64467745
Tumour rupture	24.41	21.41	8	25304	353	64473067
Malaise	24.38	21.41	250	25062	395997	64077423
Pneumonia	24.34	21.41	125	25187	559451	63913969
Syncope	24.27	21.41	16	25296	157619	64315801
Cancer pain	24.12	21.41	17	25295	4240	64469180
Treatment failure	23.91	21.41	8	25304	116808	64356612
Protein urine present	23.73	21.41	23	25289	8933	64464487
Hepatic lesion	23.53	21.41	19	25293	5805	64467615
Abnormal loss of weight	23.46	21.41	21	25291	7379	64466041
Anxiety	23.42	21.41	27	25285	202622	64270798
Depression	22.75	21.41	23	25289	183268	64290152
Intestinal metastasis	22.57	21.41	7	25305	258	64473162
Asthma	22.33	21.41	5	25307	95220	64378200
Hepatic pain	22.21	21.41	15	25297	3493	64469927
Osteosarcoma metastatic	22.16	21.41	5	25307	51	64473369
Cardiac failure congestive	21.86	21.41	12	25300	130568	64342852
Metastases to abdominal cavity	21.85	21.41	8	25304	493	64472927
Hypersensitivity	21.82	21.41	27	25285	196425	64276995
Angular cheilitis	21.80	21.41	8	25304	496	64472924
Skin disorder	21.73	21.41	39	25273	27641	64445779

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
Serine/threonine-protein kinase B-raf	Kinase	P15056	BRAF_HUMAN	INHIBITOR	IC50	7.55	CHEMBL	CHEMBL
Vascular endothelial growth factor receptor 2	Kinase	P35968	VGFR2_HUMAN	INHIBITOR	IC50	7.90	IUPHAR	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
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
Glycine receptor subunit alpha-1	Ion channel	P23415	GLRA1_HUMAN		EC50	5.74	CHEMBL
Receptor-interacting serine/threonine-protein kinase 3	Kinase	Q9Y572	RIPK3_HUMAN		Kd	6.43	CHEMBL
Platelet-derived growth factor receptor beta	Kinase	P09619	PGFRB_HUMAN		IC50	8.82	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
4031721	VANDF
CHEBI:68647	CHEBI
CHEMBL1946170	ChEMBL_ID
C559147	MESH_SUPPLEMENTAL_RECORD_UI
5891	IUPHAR_LIGAND_ID
DB08896	DRUGBANK_ID
MGN125FS9D	UNII
11167602	PUBCHEM_CID
1312397	RXNORM
193440	MMSL
28887	MMSL
d07913	MMSL
014656	NDDF
702804006	SNOMEDCT_US
703808002	SNOMEDCT_US
C2980094	UMLSCUI
1019206-88-2	SECONDARY_CAS_RN

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