RG-7103

Investigational

Approval Year

Substance Class	Protein Created by `admin` on `Wed Apr 02 02:04:14 GMT 2025` Edited by `admin` on `Wed Apr 02 02:04:14 GMT 2025`
Protein Sub Type
Sequence Type	COMPLETE
Record UNII	9TTJ40KJ7S
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

RG-7103

Common Name

English

R-7103

Preferred Name

English

RO5024118

Code

English

RO-5024118

Code

English

L-THREONINAMIDE, N-ACETYL-L-HISTIDYL-L-SERYL-L-.ALPHA.-ASPARTYL-L-ALANYL-2-METHYL-L-VALYL-L-PHENYLALANYL-L-THREONYL-L-.ALPHA.-GLUTAMYL-L-ASPARAGINYL-L-TYROSYL-L-THREONYL-L-LYSYL-L-LEUCYL-L-ARGINYL-L-LYSYL-L-GLUTAMINYL-L-NORLEUCYL-L-ALANYL-L-ALANYL-L-LYSY

Systematic Name

English

Code System Code Type Description

CAS

1001080-55-2

Created by admin on Wed Apr 02 02:04:14 GMT 2025 , Edited by admin on Wed Apr 02 02:04:14 GMT 2025

PRIMARY

PUBCHEM

90871060

Created by admin on Wed Apr 02 02:04:14 GMT 2025 , Edited by admin on Wed Apr 02 02:04:14 GMT 2025

PRIMARY

SMS_ID

100000175613

Created by admin on Wed Apr 02 02:04:14 GMT 2025 , Edited by admin on Wed Apr 02 02:04:14 GMT 2025

PRIMARY

FDA UNII

9TTJ40KJ7S

Created by admin on Wed Apr 02 02:04:14 GMT 2025 , Edited by admin on Wed Apr 02 02:04:14 GMT 2025

PRIMARY

Linkage Type	Residue Index
LYS-ASP LACTAM	1_21	1_25

Related Record Type Details


					32JI4S9U7C

VASOACTIVE INTESTINAL POLYPEPTIDE RECEPTOR 2

TARGET -> AGONIST

Related Record Type Details


					9TTJ40KJ7S

RG-7103

ACTIVE MOIETY

Comments:

RO5024118 demonstrated increased stability to neutrophil elastase compared with RO0251553. In human and guinea pig isolated airway preparations, RO5024118 induced bronchodilatory effects comparable with RO0251553 and the long-acting .BETA.-agonist salmeterol and was significantly more potent than native vasoactive intestinal peptide and the short-acting .BETA.-agonist salbutamol. In 5-HT-induced bronchoconstriction in guinea pigs, RO5024118 exhibited inhibitory activity with similar efficacy as, and longer duration than, RO0251553. In a lipopolysaccharide-mouse model, RO5024118 inhibited neutrophil and CD8(+) cells and myeloperoxidase levels. In rats, intratracheal instillation of PPE induced airway neutrophilia that was resistant to dexamethasone. Pretreatment with RO5024118 significantly inhibited PPE-induced neutrophil accumulation. These results demonstrate that RO5024118 induces dual bronchodilatory and pulmonary anti-inflammatory activity and may be beneficial in treating airway obstructive and inflammatory diseases.


					9TTJ40KJ7S

RG-7103

ACTIVE MOIETY

Comments:

Status: Withdrawn; Protocol number: NP22131; Sponsor: Hoffmann-La Roche; Brief summary: This study will assess the safety, tolerability, pharmacodynamics, and pharmacokinetics of RO5024118 following repeated inhalation in patients with moderate-to-severe Chronic Obstructive Pulmonary Disease (COPD). Patients will be randomized to receive multiple inhaled doses of R7103, as compared with placebo. The target sample size is approximately 30 individuals. Target sample size is 12.


					9TTJ40KJ7S

RG-7103

ACTIVE MOIETY

Comments:

Originator: Roche; Class: Antiasthmatic, Small molecule; Mechanism of Action: Vasoactive intestinal peptide type II receptor agonist; Highest Development Phase: Discontinued for Chronic obstructive pulmonary disease; Most Recent Event: 27 Oct 2009 Phase-I development is ongoing

Structural Modifications

Modification Type	Location Site	Location Type	Residue Modified	Extent	Fragment Name	Fragment Approval
AMINO ACID SUBSTITUTION	[1_1]		HISTIDINE	Amount:	N-ACETYLHISTIDINE	K9T7JPU4ML
AMINO ACID SUBSTITUTION	[1_17]			Amount:	NORLEUCINE	832C8OV84S
AMINO ACID SUBSTITUTION	[1_31]		THREONINE	Amount:	THREONINAMIDE	G5H9PK5HEK
AMINO_ACID_SUBSTITUTION	[1_21] [1_25]	SITE_SPECIFIC			LYS-ASP LACTAM	U3R4W875S0

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