ASTODRIMER SODIUM

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National Institutes of Health Divider Arrow

NCATS

Investigational

Description
Sources: https://clinicaltrials.gov/ct2/show/NCT01577537 | https://www.ncbi.nlm.nih.gov/pubmed/26495445 | https://clinicaltrials.gov/ct2/show/NCT00740584

Astodrimer, also known as SPL7013, a microbicide developed by Starpharm. This drug has been used in phase III clinical trials for the treatment and prevention of Bacterial Vaginosis. Starpharma conducts a meeting with US FDA related to potential approval of astodrimer in Bacterial vaginosis. In addition, SPL7013, participated in phase II clinical trials against human immunodeficiency virus (HIV) and herpes simplex virus 2 (genital herpes, HSV-2). It is known that astodrimer binds tightly to R5 gp120 in the gp120-CD4 complex, thus preventing the accrual of the requisite number of gp120-CD4 complexes across the virus-cell interface, thereby blocking virus entry.

Approval Year

Conditions

Conditions

Condition	Modality	Targets	Highest Phase	Product
Bacterial Vaginosis 2 Sources: https://clinicaltrials.gov/ct2/show/NCT01577537	Curative		Phase III 665	Unknown Approved Use Unknown

PubMed

PubMed

Title	Date	PubMed
The SPL7013 dendrimer destabilizes the HIV-1 gp120-CD4 complex.	2015-11-28	26495445
SPL7013 Gel (VivaGel®) retains potent HIV-1 and HSV-2 inhibitory activity following vaginal administration in humans.	2011	21935377
SPL7013 gel as a topical microbicide for prevention of vaginal transmission of SHIV89.6P in macaques.	2005-03	15795526

Sample Use Guides

In Vivo Use Guide

1% SPL7013 (ASTODRIMER) vaginal gel, daily for 7 days

Route of Administration: Vaginal

Substance Class	Protein Created by `admin` on `Mon Mar 31 22:53:52 GMT 2025` Edited by `admin` on `Mon Mar 31 22:53:52 GMT 2025`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	8Q3B8SV59L
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

TETRAHEXACONTASODIUM N2,N6-BIS(N2,N6-BIS(N2,N6-BIS(N2,N6-BIS(N2,N6-BIS((3,6- DISULFONAPHTHALEN-1-YLOXY)ACETYL)-L-LYSYL)-L-LYSYL)-L-LYSYL)-L-LYSYL)- N1-(DIPHENYLMETHYL)-L-LYSINAMIDE

Preferred Name

English

ASTODRIMER SODIUM

Official Name

English

Astodrimer sodium [WHO-DD]

Common Name

English

SPL-7013 SODIUM

Code

English

BRI7013 SODIUM

Code

English

BRI-7013 SODIUM

Code

English

6436

Code

English

ASTODRIMER SODIUM [USAN]

Common Name

English

Code System Code Type Description

SMS_ID

300000021737

Created by admin on Mon Mar 31 22:53:52 GMT 2025 , Edited by admin on Mon Mar 31 22:53:52 GMT 2025

PRIMARY

DRUG BANK

DBSALT002095

Created by admin on Mon Mar 31 22:53:52 GMT 2025 , Edited by admin on Mon Mar 31 22:53:52 GMT 2025

PRIMARY

ChEMBL

CHEMBL2364666

Created by admin on Mon Mar 31 22:53:52 GMT 2025 , Edited by admin on Mon Mar 31 22:53:52 GMT 2025

PRIMARY

MESH

C480351

Created by admin on Mon Mar 31 22:53:52 GMT 2025 , Edited by admin on Mon Mar 31 22:53:52 GMT 2025

PRIMARY

FDA UNII

8Q3B8SV59L

Created by admin on Mon Mar 31 22:53:52 GMT 2025 , Edited by admin on Mon Mar 31 22:53:52 GMT 2025

PRIMARY

NCI_THESAURUS

C188539

Created by admin on Mon Mar 31 22:53:52 GMT 2025 , Edited by admin on Mon Mar 31 22:53:52 GMT 2025

PRIMARY

USAN

ZZ-169

Created by admin on Mon Mar 31 22:53:52 GMT 2025 , Edited by admin on Mon Mar 31 22:53:52 GMT 2025

PRIMARY

Linkage Type	Residue Index
AMIDE BOND	16_1	1_5	2_4	4_3	8_2
AMIDE BOND	1_4	3_3	7_2	15_1
amide bridge	2_3	6_2	14_1
amide bridge	4_2	12_1
amide bridge	3_2	11_1
amide bridge	2_2	10_1
amide bridge	1_2	9_1
amide bridge	1_3	5_2	13_1

Related Record Type Details


					F8H3J9KSY9

PARENT -> SALT/SOLVATE

Amount:

Related Record Type Details


					F8H3J9KSY9

ACTIVE MOIETY

Amount:

Structural Modifications

Modification Type	Location Site	Location Type	Residue Modified	Extent	Fragment Name	Fragment Approval
AMINO_ACID_SUBSTITUTION	[1_2] [9_1]	SITE_SPECIFIC			TETRASODIUM 4-(2-(((5S)-6-(((5S)-5-AMINO-6-HYDROXY-6-OXO-HEXYL)AMINO)-5-((2-((3,6-DISULFONATO-1-NAPHTHYL)OXY)ACETYL)AMINO)-6-OXO-HEXYL)AMINO)-2-OXO-ETHOXY)NAPHTHALENE-2,7-DISULFONATE	RQ836T0UK5
AMINO_ACID_SUBSTITUTION	[3_2] [11_1]	SITE_SPECIFIC			TETRASODIUM 4-(2-(((5S)-6-(((5S)-5-AMINO-6-HYDROXY-6-OXO-HEXYL)AMINO)-5-((2-((3,6-DISULFONATO-1-NAPHTHYL)OXY)ACETYL)AMINO)-6-OXO-HEXYL)AMINO)-2-OXO-ETHOXY)NAPHTHALENE-2,7-DISULFONATE	RQ836T0UK5
AMINO_ACID_SUBSTITUTION	[2_3] [6_2] [14_1]	SITE_SPECIFIC			TETRASODIUM 4-(2-(((5S)-6-(((5S)-5-AMINO-6-(((5S)-5-AMINO-6-HYDROXY-6-OXO-HEXYL)AMINO)-6-OXO-HEXYL)AMINO)-5-((2-((3,6-DISULFONATO-1-NAPHTHYL)OXY)ACETYL)AMINO)-6-OXO-HEXYL)AMINO)-2-OXO-ETHOXY)NAPHTHALENE-2,7-DISULFONATE	LF9WH2CE4I
AMINO_ACID_SUBSTITUTION	[1_3] [5_2] [13_1]	SITE_SPECIFIC			TETRASODIUM 4-(2-(((5S)-6-(((5S)-5-AMINO-6-(((5S)-5-AMINO-6-HYDROXY-6-OXO-HEXYL)AMINO)-6-OXO-HEXYL)AMINO)-5-((2-((3,6-DISULFONATO-1-NAPHTHYL)OXY)ACETYL)AMINO)-6-OXO-HEXYL)AMINO)-2-OXO-ETHOXY)NAPHTHALENE-2,7-DISULFONATE	LF9WH2CE4I
AMINO_ACID_SUBSTITUTION	[16_1] [1_5] [2_4] [4_3] [8_2]	SITE_SPECIFIC			ASTODRIMER SODIUM MODIFIED PENTALYSINE	VOP2TX5Y69
AMINO_ACID_SUBSTITUTION	[1_4] [3_3] [7_2] [15_1]	SITE_SPECIFIC			ASTODRIMER SODIUM MODIFIED TETRALYSINE	3LCH58H5IY
AMINO_ACID_SUBSTITUTION	[1_1] [2_1] [3_1] [4_1] [5_1] [6_1] [7_1] [8_1]	SITE_SPECIFIC			TETRASODIUM 4-(2-(((5S)-5-((2-((3,6-DISULFONATO-1-NAPHTHYL)OXY)ACETYL)AMINO)-6-HYDROXY-6-OXO-HEXYL)AMINO)-2-OXO-ETHOXY)NAPHTHALENE-2,7-DISULFONATE	D8CGS7QNG5
AMINO_ACID_SUBSTITUTION	[2_2] [10_1]	SITE_SPECIFIC			TETRASODIUM 4-(2-(((5S)-6-(((5S)-5-AMINO-6-HYDROXY-6-OXO-HEXYL)AMINO)-5-((2-((3,6-DISULFONATO-1-NAPHTHYL)OXY)ACETYL)AMINO)-6-OXO-HEXYL)AMINO)-2-OXO-ETHOXY)NAPHTHALENE-2,7-DISULFONATE	RQ836T0UK5
AMINO_ACID_SUBSTITUTION	[4_2] [12_1]	SITE_SPECIFIC			TETRASODIUM 4-(2-(((5S)-6-(((5S)-5-AMINO-6-HYDROXY-6-OXO-HEXYL)AMINO)-5-((2-((3,6-DISULFONATO-1-NAPHTHYL)OXY)ACETYL)AMINO)-6-OXO-HEXYL)AMINO)-2-OXO-ETHOXY)NAPHTHALENE-2,7-DISULFONATE	RQ836T0UK5

Name	Property Type	Amount	Referenced Substance	Defining	Parameters	References
Molecular Formula	CHEMICAL
MOL_WEIGHT:NUMBER(CALCULATED)	CHEMICAL