faricimab

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Stem definition	Drug id	CAS RN
primate origin	5515	1607793-29-2

Stem definition

Drug id

CAS RN

primate origin

5515

1607793-29-2

Description:

Molecule	Description
Molfile Synonyms: faricimab faricimab-svoa vabysmo RO6867461 RG7716 faricimab (genetical recombination)	Faricimab is a humanized bispecific antibody that acts through inhibition of two pathways by binding to VEGF-A and Ang-2. By inhibiting VEGF-A, faricimab suppresses endothelial cell proliferation, neovascularization and vascular permeability. By inhibiting Ang-2, faricimab is thought to promote vascular stability and desensitize blood vessels to the effects of VEGF-A. Ang-2 levels are increased in some patients with nAMD and DME. The contribution of Ang-2 inhibition to the treatment effect and clinical response for nAMD and DME has yet to be established. Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Molfile

Synonyms:

faricimab
faricimab-svoa
vabysmo
RO6867461
RG7716
faricimab (genetical recombination)

Faricimab is a humanized bispecific antibody that acts through inhibition of two pathways by binding to VEGF-A and Ang-2. By inhibiting VEGF-A, faricimab suppresses endothelial cell proliferation, neovascularization and vascular permeability. By inhibiting Ang-2, faricimab is thought to promote vascular stability and desensitize blood vessels to the effects of VEGF-A. Ang-2 levels are increased in some patients with nAMD and DME. The contribution of Ang-2 inhibition to the treatment effect and clinical response for nAMD and DME has yet to be established.

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

Date	Agency	Company
Jan. 28, 2022	FDA	GENENTECH INC
Sept. 15, 2022	EMA	ROCHE REGISTRATION GMBH
March 28, 2022	PMDA	Chugai Pharmaceutical Co., Ltd

Date

Agency

Company

Orphan

Jan. 28, 2022

FDA

GENENTECH INC

Sept. 15, 2022

EMA

ROCHE REGISTRATION GMBH

March 28, 2022

PMDA

Chugai Pharmaceutical Co., Ltd

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
Retinal thickening	3275.49	147.70	349	2013	98	90625987
Optical coherence tomography abnormal	1790.13	147.70	191	2171	48	90626037
Visual acuity tests abnormal	577.98	147.70	67	2295	105	90625980
Vitritis	442.84	147.70	69	2293	1545	90624540
Uveitis	390.97	147.70	89	2273	15814	90610271
Iridocyclitis	373.19	147.70	67	2295	3594	90622491
Off label use	348.72	147.70	258	2104	1101994	89524091
Visual impairment	341.36	147.70	128	2234	132237	90493848
Eye inflammation	293.27	147.70	62	2300	7789	90618296
Visual acuity reduced	273.20	147.70	72	2290	23338	90602747
Endophthalmitis	269.60	147.70	53	2309	4632	90621453
Keratic precipitates	215.56	147.70	30	2332	293	90625792
Retinal haemorrhage	167.18	147.70	37	2325	5727	90620358
Retinal occlusive vasculitis	166.63	147.70	23	2339	210	90625875

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

Retinal thickening

3275.49

147.70

349

2013

90625987

Optical coherence tomography abnormal

1790.13

147.70

191

2171

90626037

Visual acuity tests abnormal

577.98

147.70

2295

105

90625980

Vitritis

442.84

147.70

2293

1545

90624540

Uveitis

390.97

147.70

2273

15814

90610271

Iridocyclitis

373.19

147.70

2295

3594

90622491

Off label use

348.72

147.70

258

2104

1101994

89524091

Visual impairment

341.36

147.70

128

2234

132237

90493848

Eye inflammation

293.27

147.70

2300

7789

90618296

Visual acuity reduced

273.20

147.70

2290

23338

90602747

Endophthalmitis

269.60

147.70

2309

4632

90621453

Keratic precipitates

215.56

147.70

2332

293

90625792

Retinal haemorrhage

167.18

147.70

2325

5727

90620358

Retinal occlusive vasculitis

166.63

147.70

2339

210

90625875

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
Retinal thickening	2377.91	181.26	269	1365	139	42619562
Optical coherence tomography abnormal	1293.96	181.26	144	1490	37	42619664
Visual acuity tests abnormal	341.15	181.26	41	1593	56	42619645
Off label use	263.48	181.26	204	1430	638131	41981570
Visual impairment	245.77	181.26	83	1551	43030	42576671

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

Retinal thickening

2377.91

181.26

269

1365

139

42619562

Optical coherence tomography abnormal

1293.96

181.26

144

1490

42619664

Visual acuity tests abnormal

341.15

181.26

1593

42619645

Off label use

263.48

181.26

204

1430

638131

41981570

Visual impairment

245.77

181.26

1551

43030

42576671

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
Retinal thickening	1104.83	121.56	125	2317	185	110586672
Optical coherence tomography abnormal	998.12	121.56	107	2335	55	110586802
Vitritis	513.46	121.56	82	2360	2571	110584286
Iridocyclitis	468.28	121.56	84	2358	5324	110581533
Uveitis	452.77	121.56	103	2339	21607	110565250
Off label use	375.14	121.56	285	2157	1499900	109086957
Visual acuity tests abnormal	320.00	121.56	39	2403	140	110586717
Endophthalmitis	318.56	121.56	65	2377	8122	110578735
Eye inflammation	305.42	121.56	64	2378	9107	110577750
No adverse event	254.14	121.56	85	2357	73754	110513103
Retinal haemorrhage	235.43	121.56	52	2390	9449	110577408
Visual acuity reduced	221.07	121.56	63	2379	32110	110554747
Visual impairment	214.73	121.56	88	2354	134340	110452517
Retinal occlusive vasculitis	201.78	121.56	27	2415	230	110586627
Keratic precipitates	180.95	121.56	27	2415	529	110586328
Anterior chamber inflammation	179.38	121.56	28	2414	747	110586110
Retinal pigment epithelial tear	152.88	121.56	23	2419	477	110586380
Death	137.60	121.56	117	2325	698752	109888105
Iritis	123.68	121.56	27	2415	4625	110582232

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

Retinal thickening

1104.83

121.56

125

2317

185

110586672

Optical coherence tomography abnormal

998.12

121.56

107

2335

110586802

Vitritis

513.46

121.56

2360

2571

110584286

Iridocyclitis

468.28

121.56

2358

5324

110581533

Uveitis

452.77

121.56

103

2339

21607

110565250

Off label use

375.14

121.56

285

2157

1499900

109086957

Visual acuity tests abnormal

320.00

121.56

2403

140

110586717

Endophthalmitis

318.56

121.56

2377

8122

110578735

Eye inflammation

305.42

121.56

2378

9107

110577750

No adverse event

254.14

121.56

2357

73754

110513103

Retinal haemorrhage

235.43

121.56

2390

9449

110577408

Visual acuity reduced

221.07

121.56

2379

32110

110554747

Visual impairment

214.73

121.56

2354

134340

110452517

Retinal occlusive vasculitis

201.78

121.56

2415

230

110586627

Keratic precipitates

180.95

121.56

2415

529

110586328

Anterior chamber inflammation

179.38

121.56

2414

747

110586110

Retinal pigment epithelial tear

152.88

121.56

2419

477

110586380

Death

137.60

121.56

117

2325

698752

109888105

Iritis

123.68

121.56

2415

4625

110582232

Pharmacologic Action:

Source	Code	Description
ATC	S01LA09	SENSORY ORGANS OPHTHALMOLOGICALS OCULAR VASCULAR DISORDER AGENTS Antineovascularisation agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D006131	Growth Inhibitors
MeSH PA	D006133	Growth Substances
MeSH PA	D020533	Angiogenesis Inhibitors
CHEBI has role	CHEBI:66981	ophthalmology drug

Source

Code

Description

ATC

S01LA09

SENSORY ORGANS
OPHTHALMOLOGICALS
OCULAR VASCULAR DISORDER AGENTS
Antineovascularisation agents

MeSH PA

D000970

Antineoplastic Agents

MeSH PA

D006131

Growth Inhibitors

MeSH PA

D006133

Growth Substances

MeSH PA

D020533

Angiogenesis Inhibitors

CHEBI has role

CHEBI:66981

ophthalmology drug

Disease	Relation	SNOMED_ID	DOID
Macular edema due to diabetes mellitus	indication	312912001	DOID:9191
Exudative age-related macular degeneration	indication	414173003	DOID:10873
Uveitis	contraindication	128473001	DOID:13141
Ocular or periocular infection	contraindication	715266002

Disease

Relation

SNOMED_ID

DOID

Macular edema due to diabetes mellitus

indication

312912001

DOID:9191

Exudative age-related macular degeneration

indication

414173003

DOID:10873

Uveitis

contraindication

128473001

DOID:13141

Ocular or periocular infection

contraindication

715266002

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Vascular endothelial growth factor A	Secreted	P15692	VEGFA_HUMAN	BINDING AGENT	Kd	8.76		DRUG LABEL	DRUG LABEL
Angiopoietin-2	Secreted	O15123	ANGP2_HUMAN	BINDING AGENT	Kd	7.70		DRUG LABEL	DRUG LABEL

Target

Class

Pharos

UniProt

Action

Type

Activity value
(-log[M])

Mechanism
action

Bioact source

MoA source

Vascular endothelial growth factor A

Secreted

P15692

VEGFA_HUMAN

BINDING AGENT

8.76

DRUG LABEL

Angiopoietin-2

Secreted

O15123

ANGP2_HUMAN

BINDING AGENT

7.70

DRUG LABEL

External reference:

ID	Source
CHEBI:757201	CHEBI
CHEMBL4297750	ChEMBL_ID
C000723200	MESH_SUPPLEMENTAL_RECORD_UI
11420	IUPHAR_LIGAND_ID
DB15303	DRUGBANK_ID
278201000202106	SNOMEDCT_US
4041143	VANDF
4041144	VANDF
C5139890	UMLSCUI
D11516	KEGG_DRUG
10563	INN_ID
91827367	PUBCHEM_CID
358850	MMSL
40656	MMSL
018943	NDDF
QC4F7FKK7I	UNII
2591519	RXNORM

Source

CHEBI:757201

CHEBI

CHEMBL4297750

ChEMBL_ID

C000723200

MESH_SUPPLEMENTAL_RECORD_UI

11420

IUPHAR_LIGAND_ID

DB15303

DRUGBANK_ID

278201000202106