Trastuzumab Vedotin

Investigational

Approval Year

Substance Class	Protein
Protein Type	MONOCLONAL ANTIBODY CONJUGATE
Protein Sub Type	IGG1\|TOXIN CONJUGATE
Sequence Origin	HUMANIZED MOUSE
Sequence Type	COMPLETE
Record UNII	W95G28K44S
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

Trastuzumab Vedotin

Official Name

English

MRG-002

Preferred Name

English

Immunoglobulin G1-kappa, anti-[Homo sapiens ERBB2 (receptor tyrosine-protein kinase erbB-2, epidermal growth factor receptor 2, EGFR2, HER2, HER-2, p185c-erbB2, NEU, CD340)], humanized monoclonal antibody; conjugated to auristatin E

Common Name

English

MRG 002 [WHO-DD]

Common Name

English

TRASTUZUMAB--VCMMAE CONJUGATE

Common Name

English

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Classification Tree

Code System

Code

Designated

FDA ORPHAN DRUG

898822

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Code System

Code

Type

Description

SMS_ID

300000050047

PRIMARY

INN

12531

PRIMARY

NCI_THESAURUS

C174205

PRIMARY

CAS

2740607-04-7

PRIMARY

FDA UNII

W95G28K44S

PRIMARY

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Subunit 0

Subunit 1

Subunit 2

Subunit 3

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From	To
4_134	4_194
4_23	4_88
3_134	3_194
3_23	3_88
2_370	2_428

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Glycosylation Type

MAMMALIAN

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Glycosylation Link Type	Site
N	1_300
N	2_300

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Related Record

Type

Details


					Q3606FDE0B

VEDOTIN FRAGMENT

CONJUGATE COMPONENT->CONJUGATE

Amount:


					6603L01WUR

Cysteinyl vedotin

CONJUGATE COMPONENT->CONJUGATE

Amount:


					P188ANX8CK

TRASTUZUMAB

CONJUGATE COMPONENT->CONJUGATE

Amount:


					7J9Y28299R

RECEPTOR TYROSINE-PROTEIN KINASE ERBB-2

TARGET->CONJUGATED TOXIN

Comments:

MRG002 potently inhibited proliferation of HER2 expressing cancer cells in vitro with IC50 ranged from 1.8±0.8 to 59.9±8.9 ng/mL,

Amount:

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Related Record

Type

Details


					W95G28K44S

Trastuzumab Vedotin

ACTIVE MOIETY

Amount:

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Structural Modifications

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Modification Type	Location Site	Location Type	Residue Modified	Extent	Fragment Name	Fragment Approval
AMINO_ACID_SUBSTITUTION		RESIDUE_SPECIFIC	Cysteine		Cysteinyl vedotin	6603L01WUR
AMINO ACID REMOVAL	[1_450] [2_450]	C-TERMINUS		Amount: major	LYSINE	K3Z4F929H6
AMINO_ACID_SUBSTITUTION				Amount: minor	PIDOLIC ACID	SZB83O1W42

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Name	Property Type	Amount	Referenced Substance	Defining	Parameters	References
Molecular Formula	CHEMICAL	ESTIMATED C6460H9954N1724O2014S44
MOL_WEIGHT:NUMBER(CALCULATED)	CHEMICAL	ESTIMATED 145000 Da (average)

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