belantamab mafodotin

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Stem definition	Drug id	CAS RN
antitumor, monoclonal antibodies	5405	2050232-20-5

Stem definition

Drug id

CAS RN

antitumor, monoclonal antibodies

5405

2050232-20-5

Description:

Molecule	Description
Molfile Synonyms: belantamab mafodotin belantamab belantamab mafodotin-blmf blenrep anti-BCMA-ADC GSK2857914 GSK-2857916 J6M0-mcMMAF	Belantamab mafodotin-blmf is an antibody-drug conjugate (ADC). The antibody component is an afucosylated IgG1 directed against BCMA, a protein expressed on normal B lymphocytes and multiple myeloma cells. The small molecule component is MMAF, a microtubule inhibitor. Upon binding to BCMA, belantamab mafodotin-blmf is internalized followed by release of MMAF via proteolytic cleavage. The released MMAF intracellularly disrupts the microtubule network, leading to cell cycle arrest and apoptosis. Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Molfile

Synonyms:

belantamab mafodotin
belantamab
belantamab mafodotin-blmf
blenrep
anti-BCMA-ADC
GSK2857914
GSK-2857916
J6M0-mcMMAF

Belantamab mafodotin-blmf is an antibody-drug conjugate (ADC). The antibody component is an afucosylated IgG1 directed against BCMA, a protein expressed on normal B lymphocytes and multiple myeloma cells. The small molecule component is MMAF, a microtubule inhibitor. Upon binding to BCMA, belantamab mafodotin-blmf is internalized followed by release of MMAF via proteolytic cleavage. The released MMAF intracellularly disrupts the microtubule network, leading to cell cycle arrest and apoptosis.

Molecular weight:
Formula:
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Date	Agency	Company	Orphan
May 8, 2020	FDA	GLAXOSMITHKLINE
Aug. 25, 2020	EMA	GlaxoSmithKline (Ireland) Limited

Date

Agency

Company

Orphan

May 8, 2020

FDA

GLAXOSMITHKLINE

Aug. 25, 2020

EMA

GlaxoSmithKline (Ireland) 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
Keratopathy	904.74	65.45	106	928	602	90626811
Visual acuity reduced	521.97	65.45	104	930	23306	90604107
Night blindness	332.43	65.45	42	992	463	90626950
Dry eye	203.80	65.45	58	976	57873	90569540
Foreign body sensation in eyes	144.34	65.45	26	1008	3274	90624139
Death	121.83	65.45	71	963	456480	90170933
Ocular toxicity	106.10	65.45	17	1017	1060	90626353
Photophobia	100.81	65.45	27	1007	21242	90606171

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

Keratopathy

904.74

65.45

106

928

602

90626811

Visual acuity reduced

521.97

65.45

104

930

23306

90604107

Night blindness

332.43

65.45

992

463

90626950

Dry eye

203.80

65.45

976

57873

90569540

Foreign body sensation in eyes

144.34

65.45

1008

3274

90624139

Death

121.83

65.45

963

456480

90170933

Ocular toxicity

106.10

65.45

1017

1060

90626353

Photophobia

100.81

65.45

1007

21242

90606171

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
Keratopathy	1137.26	56.87	144	1131	554	42619506
Visual acuity reduced	527.09	56.87	118	1157	17432	42602628
Night blindness	234.36	56.87	32	1243	231	42619829
Dry eye	180.74	56.87	49	1226	15457	42604603
Punctate keratitis	126.65	56.87	20	1255	421	42619639
Corneal epithelial microcysts	119.79	56.87	13	1262	3	42620057
Corneal epithelium defect	91.30	56.87	15	1260	407	42619653
Photophobia	73.07	56.87	21	1254	8098	42611962
Foreign body sensation in eyes	72.83	56.87	14	1261	941	42619119
Corneal disorder	71.38	56.87	14	1261	1045	42619015
Death	69.43	56.87	77	1198	471108	42148952
Ocular toxicity	57.79	56.87	10	1265	372	42619688

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

Keratopathy

1137.26

56.87

144

1131

554

42619506

Visual acuity reduced

527.09

56.87

118

1157

17432

42602628

Night blindness

234.36

56.87

1243

231

42619829

Dry eye

180.74

56.87

1226

15457

42604603

Punctate keratitis

126.65

56.87

1255

421

42619639

Corneal epithelial microcysts

119.79

56.87

1262

42620057

Corneal epithelium defect

91.30

56.87

1260

407

42619653

Photophobia

73.07

56.87

1254

8098

42611962

Foreign body sensation in eyes

72.83

56.87

1261

941

42619119

Corneal disorder

71.38

56.87

1261

1045

42619015

Death

69.43

56.87

1198

471108

42148952

Ocular toxicity

57.79

56.87

1265

372

42619688

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
Keratopathy	1667.27	47.11	206	1763	1167	110586163
Visual acuity reduced	875.74	47.11	182	1787	31991	110555339
Night blindness	432.18	47.11	57	1912	552	110586778
Dry eye	327.75	47.11	92	1877	55701	110531629
Foreign body sensation in eyes	182.27	47.11	34	1935	3300	110584030
Ocular toxicity	170.17	47.11	28	1941	1310	110586020
Corneal epithelial microcysts	150.99	47.11	17	1952	32	110587298
Punctate keratitis	144.67	47.11	24	1945	1180	110586150
Photophobia	130.65	47.11	38	1931	25733	110561597
Corneal epithelium defect	122.44	47.11	20	1949	892	110586438
Corneal disorder	71.83	47.11	15	1954	2582	110584748
Death	60.73	47.11	68	1901	698801	109888529
Corneal cyst	56.56	47.11	6	1963	4	110587326
Visual impairment	56.22	47.11	33	1936	134395	110452935
Plasma cell myeloma refractory	52.12	47.11	11	1958	1990	110585340
Plasmacytoma	51.26	47.11	13	1956	5249	110582081

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

Keratopathy

1667.27

47.11

206

1763

1167

110586163

Visual acuity reduced

875.74

47.11

182

1787

31991

110555339

Night blindness

432.18

47.11

1912

552

110586778

Dry eye

327.75

47.11

1877

55701

110531629

Foreign body sensation in eyes

182.27

47.11

1935

3300

110584030

Ocular toxicity

170.17

47.11

1941

1310

110586020

Corneal epithelial microcysts

150.99

47.11

1952

110587298

Punctate keratitis

144.67

47.11

1945

1180

110586150

Photophobia

130.65

47.11

1931

25733

110561597

Corneal epithelium defect

122.44

47.11

1949

892

110586438

Corneal disorder

71.83

47.11

1954

2582

110584748

Death

60.73

47.11

1901

698801

109888529

Corneal cyst

56.56

47.11

1963

110587326

Visual impairment

56.22

47.11

1936

134395

110452935

Plasma cell myeloma refractory

52.12

47.11

1958

1990

110585340

Plasmacytoma

51.26

47.11

1956

5249

110582081

Source	Code	Description
ATC	L01FX15	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES Other monoclonal antibodies and antibody drug conjugates
CHEBI has role	CHEBI:35610	antineoplastic agent

Source

Code

Description

ATC

L01FX15

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
MONOCLONAL ANTIBODIES AND ANTIBODY DRUG CONJUGATES
Other monoclonal antibodies and antibody drug conjugates

CHEBI has role

CHEBI:35610

antineoplastic agent

Disease	Relation	SNOMED_ID	DOID
Multiple myeloma	indication	109989006	DOID:9538
Relapse multiple myeloma	indication

Disease

Relation

SNOMED_ID

DOID

Multiple myeloma

indication

109989006

DOID:9538

Relapse multiple myeloma

indication

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
IgG receptor FcRn large subunit p51	Membrane receptor	P55899	FCGRN_HUMAN	BINDING AGENT	Kd	7.28	DRUG LABEL	DRUG LABEL
High affinity immunoglobulin gamma Fc receptor I	Membrane receptor	P12314	FCGR1_HUMAN	BINDING AGENT	Kd	8.15	DRUG LABEL	DRUG LABEL
Low affinity immunoglobulin gamma Fc region receptor III-A	Membrane receptor	P08637	FCG3A_HUMAN	BINDING AGENT	Kd	7.55	DRUG LABEL	DRUG LABEL
Tumor necrosis factor receptor superfamily member 17	Tumour-associated antigen	Q02223	TNR17_HUMAN	BINDING AGENT	Kd	9	SCIENTIFIC LITERATURE	DRUG LABEL

Target

Class

Pharos

UniProt

Action

Type

Activity value
(-log[M])

Mechanism
action

Bioact source

MoA source

IgG receptor FcRn large subunit p51

Membrane receptor

P55899

FCGRN_HUMAN

BINDING AGENT

7.28

DRUG LABEL

High affinity immunoglobulin gamma Fc receptor I

Membrane receptor

P12314

FCGR1_HUMAN

BINDING AGENT

8.15

DRUG LABEL

Low affinity immunoglobulin gamma Fc region receptor III-A

Membrane receptor

P08637

FCG3A_HUMAN

BINDING AGENT

7.55

DRUG LABEL

Tumor necrosis factor receptor superfamily member 17

Tumour-associated antigen

Q02223

TNR17_HUMAN

BINDING AGENT

SCIENTIFIC LITERATURE

DRUG LABEL

External reference:

ID	Source
D11595	KEGG_DRUG
DB1041CXDG	UNII
2061894-48-0	SECONDARY_CAS_RN
4039621	VANDF
4039622	VANDF
C5227411	UMLSCUI
CHEBI:757615	CHEBI
CHEMBL4298209	ChEMBL_ID
DB15719	DRUGBANK_ID
CHEMBL4298208	ChEMBL_ID
10754	INN_ID
C000631691	MESH_SUPPLEMENTAL_RECORD_UI
11117	IUPHAR_LIGAND_ID
895362005	SNOMEDCT_US
896748005	SNOMEDCT_US
10797	INN_ID
337068	MMSL
38715	MMSL
d09613	MMSL
018466	NDDF
2387833	RXNORM

Source

D11595

KEGG_DRUG

DB1041CXDG

UNII

2061894-48-0

SECONDARY_CAS_RN

4039621

VANDF

4039622

VANDF

C5227411