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

Stem definition	Drug id	CAS RN
synthetic derivatives of dolastatin series	4964	914088-09-8

Description:

Molecule	Description
Synonyms: brentuximab vedotin adcetris SGN-35 cAC10-vcMMAE brentuximab vedotin (genetical recombination)	a CD30-directed antibody-drug conjugate consisting of three components: the chimeric IgG1 antibody cAC10, specific for human CD30, the microtubule disrupting agent MMAE, and a protease-cleavable linker that covalently attaches MMAE to cAC10 Molecular weight: Formula: Brentuximab(C68H106N11O15S)3-5 CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

brentuximab vedotin
adcetris
SGN-35
cAC10-vcMMAE
brentuximab vedotin (genetical recombination)

a CD30-directed antibody-drug conjugate consisting of three components: the chimeric IgG1 antibody cAC10, specific for human CD30, the microtubule disrupting agent MMAE, and a protease-cleavable linker that covalently attaches MMAE to cAC10

Molecular weight:
Formula: Brentuximab(C68H106N11O15S)3-5
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

Date	Agency	Company
Oct. 25, 2012	EMA	Takeda Pharma A/S
Aug. 19, 2011	FDA	SEATTLE GENETICS
Jan. 17, 2014	PMDA	Takeda Pharmaceutical Company Limited

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
Febrile neutropenia	255.64	27.29	149	5593	118300	63364980
Neuropathy peripheral	234.73	27.29	139	5603	113528	63369752
Off label use	152.60	27.29	240	5502	674222	62809058
Neutropenia	150.20	27.29	125	5617	174880	63308400
Disease progression	99.60	27.29	85	5657	122673	63360607
Pneumocystis jirovecii pneumonia	95.49	27.29	41	5701	16873	63466407
Polyneuropathy	87.78	27.29	37	5705	14552	63468728
Thrombocytopenia	82.61	27.29	84	5658	151073	63332207
Pyrexia	71.33	27.29	141	5601	470337	63012943
Neutrophil count decreased	53.89	27.29	43	5699	56363	63426917
Ileus	52.65	27.29	26	5716	14699	63468581
Peripheral sensory neuropathy	48.52	27.29	20	5722	7431	63475849
Myelosuppression	46.15	27.29	28	5714	23675	63459605
Pancytopenia	44.23	27.29	49	5693	96884	63386396
Pneumonitis	42.79	27.29	31	5711	35191	63448089
Malignant neoplasm progression	41.82	27.29	44	5698	82077	63401203
Procalcitonin abnormal	41.55	27.29	6	5736	18	63483262
Peripheral motor neuropathy	40.59	27.29	12	5730	1669	63481611
Tumour lysis syndrome	38.59	27.29	18	5724	8972	63474308
Sepsis	37.66	27.29	57	5685	153066	63330214
Cytopenia	37.11	27.29	19	5723	11582	63471698
Blood uric acid increased	36.97	27.29	15	5727	5352	63477928
Mucosal inflammation	36.96	27.29	32	5710	46896	63436384
Gamma-glutamyltransferase abnormal	36.55	27.29	8	5734	331	63482949
Cytomegalovirus colitis	36.52	27.29	12	5730	2360	63480920
White blood cell count decreased	33.09	27.29	51	5691	139053	63344227
Weight decreased	32.55	27.29	75	5667	276723	63206557
Blood lactate dehydrogenase abnormal	30.35	27.29	7	5735	368	63482912
Neurotoxicity	30.35	27.29	19	5723	16971	63466309
Tumour flare	30.11	27.29	7	5735	381	63482899
Ectropion	29.28	27.29	6	5736	180	63483100
Anaemia	28.62	27.29	74	5668	293356	63189924
Headache	28.31	27.29	11	5731	633230	62850050
Chronic inflammatory demyelinating polyradiculoneuropathy	27.93	27.29	7	5735	524	63482756
Serum ferritin abnormal	27.73	27.29	6	5736	235	63483045
Dermatitis exfoliative generalised	27.46	27.29	11	5731	3796	63479484

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
Neuropathy peripheral	177.18	21.65	148	7749	83115	34865919
Off label use	173.71	21.65	325	7572	419199	34529835
Febrile neutropenia	145.09	21.65	166	7731	136683	34812351
Cytomegalovirus chorioretinitis	109.10	21.65	38	7859	3551	34945483
Disease progression	102.56	21.65	124	7773	107953	34841081
Polyneuropathy	96.63	21.65	53	7844	14843	34934191
Neutropenia	88.54	21.65	140	7757	156638	34792396
Pneumocystis jirovecii pneumonia	73.10	21.65	49	7848	19661	34929373
Pyrexia	68.83	21.65	197	7700	332816	34616218
Endocarditis noninfective	65.29	21.65	13	7884	127	34948907
Peripheral sensory neuropathy	60.91	21.65	30	7867	6730	34942304
Neutrophil count decreased	55.62	21.65	63	7834	51041	34897993
Acute myeloid leukaemia	55.06	21.65	40	7857	18230	34930804
Therapy partial responder	50.98	21.65	30	7867	9586	34939448
Malignant neoplasm progression	47.32	21.65	77	7820	87969	34861065
Myositis	47.14	21.65	31	7866	12039	34936995
Thrombocytopenia	46.18	21.65	106	7791	156141	34792893
Guillain-Barre syndrome	46.04	21.65	24	7873	6063	34942971
Cutaneous T-cell lymphoma	45.64	21.65	16	7881	1522	34947512
Blindness	43.32	21.65	32	7865	14954	34934080
Peripheral motor neuropathy	42.96	21.65	16	7881	1810	34947224
Cytomegalovirus infection	42.51	21.65	40	7857	26095	34922939
Molluscum contagiosum	40.28	21.65	10	7887	282	34948752
Anaplastic large-cell lymphoma	39.65	21.65	8	7889	84	34948950
Type IV hypersensitivity reaction	39.06	21.65	14	7883	1420	34947614
Myelosuppression	36.24	21.65	32	7865	19233	34929801
Cancer fatigue	34.23	21.65	7	7890	79	34948955
Sepsis	33.67	21.65	98	7799	166463	34782571
Pneumonitis	30.61	21.65	38	7859	33840	34915194
Second primary malignancy	30.17	21.65	20	7877	7866	34941168
Hepatitis viral	29.01	21.65	9	7888	584	34948450
Septic shock	28.46	21.65	55	7842	71779	34877255
Peripheral sensorimotor neuropathy	27.06	21.65	11	7886	1571	34947463
Product use in unapproved indication	26.52	21.65	72	7825	117427	34831607
Neutropenic sepsis	26.16	21.65	23	7874	13744	34935290
Tumour lysis syndrome	25.63	21.65	25	7872	17034	34932000
Peripheral T-cell lymphoma unspecified recurrent	25.48	21.65	5	7892	45	34948989
Gamma-glutamyltransferase abnormal	24.85	21.65	7	7890	324	34948710
Drug interaction	24.85	21.65	10	7887	225936	34723098
Hypogonadism	23.31	21.65	11	7886	2244	34946790
Adenocarcinoma gastric	22.56	21.65	9	7888	1224	34947810
Febrile bone marrow aplasia	22.53	21.65	17	7880	8192	34940842
Demyelinating polyneuropathy	22.44	21.65	9	7888	1242	34947792
Blood alkaline phosphatase abnormal	22.20	21.65	7	7890	479	34948555
Anaplastic large cell lymphoma T- and null-cell types refractory	22.19	21.65	3	7894	0	34949034
Pancytopenia	22.16	21.65	59	7838	95098	34853936
Visual acuity reduced transiently	21.78	21.65	5	7892	100	34948934

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
Febrile neutropenia	328.24	20.98	276	11963	230723	79501426
Neuropathy peripheral	327.11	20.98	226	12013	141079	79591070
Off label use	238.15	20.98	464	11775	906751	78825398
Disease progression	214.75	20.98	197	12042	184165	79547984
Neutropenia	205.23	20.98	236	12003	287474	79444675
Pneumocystis jirovecii pneumonia	158.42	20.98	84	12155	32424	79699725
Polyneuropathy	127.91	20.98	66	12173	24085	79708064
Neutrophil count decreased	124.24	20.98	108	12131	93851	79638298
Thrombocytopenia	115.82	20.98	171	12068	265088	79467061
Pyrexia	115.66	20.98	293	11946	678416	79053733
Peripheral sensory neuropathy	106.63	20.98	48	12191	12985	79719164
Cytomegalovirus chorioretinitis	103.84	20.98	37	12202	5453	79726696
Malignant neoplasm progression	89.06	20.98	107	12132	135883	79596266
Myelosuppression	84.93	20.98	61	12178	40235	79691914
Sepsis	70.05	20.98	138	12101	269290	79462859
Cytomegalovirus infection	68.72	20.98	55	12184	42589	79689560
Endocarditis noninfective	63.80	20.98	13	12226	218	79731931
Guillain-Barre syndrome	57.77	20.98	28	12211	8937	79723212
Tumour lysis syndrome	56.85	20.98	39	12200	23900	79708249
Acute myeloid leukaemia	56.62	20.98	43	12196	30842	79701307
Pancytopenia	53.19	20.98	93	12146	165652	79566497
Cancer fatigue	49.17	20.98	10	12229	166	79731983
Pneumonitis	48.42	20.98	53	12186	60807	79671342
Therapy partial responder	47.71	20.98	31	12208	17366	79714783
Pain	45.27	20.98	26	12213	703776	79028373
Myositis	44.98	20.98	31	12208	19137	79713012
White blood cell count decreased	43.60	20.98	92	12147	188196	79543953
Peripheral motor neuropathy	42.92	20.98	17	12222	3350	79728799
Chronic inflammatory demyelinating polyradiculoneuropathy	42.69	20.98	13	12226	1172	79730977
Septic shock	42.13	20.98	71	12168	122730	79609419
Hyperthermia	41.92	20.98	29	12210	18008	79714141
Graft versus host disease	41.76	20.98	27	12212	14999	79717150
Anaemia	41.46	20.98	156	12083	444859	79287290
Peripheral sensorimotor neuropathy	41.19	20.98	16	12223	2994	79729155
Anaplastic large-cell lymphoma	40.68	20.98	9	12230	227	79731922
Headache	39.46	20.98	26	12213	653746	79078403
Cutaneous T-cell lymphoma	39.24	20.98	15	12224	2688	79729461
Mucosal inflammation	39.19	20.98	53	12186	75527	79656622
Molluscum contagiosum	39.00	20.98	10	12229	479	79731670
Blood lactate dehydrogenase increased	38.12	20.98	38	12201	39132	79693017
Ileus	36.36	20.98	31	12208	26180	79705969
Ileus paralytic	36.24	20.98	21	12218	9599	79722550
Drug interaction	35.32	20.98	10	12229	415173	79316976
Febrile bone marrow aplasia	35.21	20.98	23	12216	12997	79719152
Neutropenic sepsis	33.50	20.98	30	12209	27034	79705115
Joint swelling	33.29	20.98	3	12236	288643	79443506
Type IV hypersensitivity reaction	33.27	20.98	15	12224	4066	79728083
Arthralgia	32.81	20.98	24	12215	571779	79160370
Drug hypersensitivity	32.19	20.98	4	12235	298912	79433237
Product use in unapproved indication	31.39	20.98	97	12142	250262	79481887
Second primary malignancy	30.85	20.98	22	12217	14328	79717821
Peripheral swelling	30.57	20.98	3	12236	269614	79462535
Multiple organ dysfunction syndrome	30.46	20.98	61	12178	120185	79611964
General physical health deterioration	30.31	20.98	102	12137	275136	79457013
Hypogonadism	30.05	20.98	11	12228	1749	79730400
Neoplasm progression	29.50	20.98	38	12201	51644	79680505
Lymphoma	29.14	20.98	23	12216	17437	79714712
Dizziness	29.04	20.98	23	12216	526418	79205731
Venoocclusive disease	28.61	20.98	14	12225	4559	79727590
Blindness	28.48	20.98	28	12211	28355	79703794
Cytomegalovirus colitis	28.29	20.98	14	12225	4671	79727478
Peripheral T-cell lymphoma unspecified recurrent	27.31	20.98	5	12234	46	79732103
Hepatitis viral	27.30	20.98	9	12230	1049	79731100
Acute respiratory distress syndrome	26.10	20.98	33	12206	44034	79688115
Cytopenia	26.03	20.98	23	12216	20360	79711789
Platelet count decreased	25.87	20.98	77	12162	194587	79537562
Bicytopenia	25.40	20.98	13	12226	4657	79727492
Dermatitis exfoliative generalised	25.16	20.98	15	12224	7226	79724923
Haemophagocytic lymphohistiocytosis	24.67	20.98	23	12216	21814	79710335
Hypertension	24.62	20.98	10	12229	330982	79401167
Nasopharyngitis	23.75	20.98	5	12234	253876	79478273
Anaplastic large cell lymphoma T- and null-cell types refractory	23.35	20.98	3	12236	0	79732149
Abdominal discomfort	23.32	20.98	5	12234	250722	79481427
Hyperglycaemia	23.22	20.98	40	12199	70295	79661854
Blood uric acid increased	23.16	20.98	18	12221	13342	79718807
Anaphylactic shock	22.99	20.98	28	12211	35968	79696181
Adenocarcinoma gastric	22.82	20.98	9	12230	1752	79730397
Leukopenia	22.52	20.98	53	12186	116460	79615689
Peripheral T-cell lymphoma unspecified	22.45	20.98	7	12232	683	79731466
Stem cell transplant	22.16	20.98	11	12228	3693	79728456
Aplasia	21.60	20.98	14	12225	7806	79724343
Ectropion	21.16	20.98	6	12233	422	79731727

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01FX05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES Other monoclonal antibodies and antibody drug conjugates
FDA CS	M0028142	Immunoconjugates
FDA PE	N0000175085	Microtubule Inhibition
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D000074322	Antineoplastic Agents, Immunological
MeSH PA	D018796	Immunoconjugates
MeSH PA	D007155	Immunologic Factors
MeSH PA	D000922	Immunotoxins
MeSH PA	D009676	Noxae
FDA MoA	N0000182966	CD30-directed Antibody Interactions
FDA EPC	N0000182967	CD30-directed Immunoconjugate

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

Disease	Relation	SNOMED_ID
CD30-positive peripheral T-cell lymphoma	indication	109977009
Hodgkin's disease	indication	118599009
Cutaneous Tcell lymphoma	indication	400122007
Anaplastic large T-cell systemic malignant lymphoma	indication	404134006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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])	Mechanism action	Bioact source	MoA source
Tumor necrosis factor receptor superfamily member 8	Membrane receptor	P28908	TNR8_HUMAN	BINDING AGENT				DRUG LABEL	DRUG LABEL
Tubulin beta	Tumour-associated antigen	P07437 Q9H4B7 Q13885 Q9BVA1 Q13509 P04350 P68371 Q9BUF5 Q3ZCM7	TBB5_HUMAN TBB1_HUMAN TBB2A_HUMAN TBB2B_HUMAN TBB3_HUMAN TBB4A_HUMAN TBB4B_HUMAN TBB6_HUMAN TBB8_HUMAN	INHIBITOR				DRUG LABEL	DRUG LABEL

External reference:

ID	Source
D09587	KEGG_DRUG
4031047	VUID
N0000183555	NUI
4031047	VANDF
CHEMBL1742994	ChEMBL_ID
6772	IUPHAR_LIGAND_ID
DB08870	DRUGBANK_ID
1147320	RXNORM
185268	MMSL
28063	MMSL
d07799	MMSL
013904	NDDF
713395006	SNOMEDCT_US
714671006	SNOMEDCT_US
C2973446	UMLSCUI
D000079963	MESH_DESCRIPTOR_UI
9144	INN_ID
117723179	PUBCHEM_CID
7XL5ISS668	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ADCETRIS	HUMAN PRESCRIPTION DRUG LABEL	1	51144-050	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	50 mg	INTRAVENOUS	BLA	27 sections
ADCETRIS	HUMAN PRESCRIPTION DRUG LABEL	1	51144-050	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	50 mg	INTRAVENOUS	BLA	27 sections
ADCETRIS	HUMAN PRESCRIPTION DRUG LABEL	1	51144-050	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	50 mg	INTRAVENOUS	BLA	27 sections
ADCETRIS	HUMAN PRESCRIPTION DRUG LABEL	1	51144-050	INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION	50 mg	INTRAVENOUS	BLA	27 sections