VELDOREOTIDE ACETATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C60H74N12O10.C2H4O2
Molecular Weight	1183.3559
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(O)=O.[H][C@]3(CC1=CNC2=C1C=CC=C2)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC6=CC=CC=C6)NC(=O)CCCNC(=O)CCCN(CC(N)=O)C(=O)[C@H](CC7=CC=CC=C7)NC(=O)[C@@]([H])(NC(=O)[C@H](CCCCN)NC3=O)[C@@H](C)O

InChI

InChIKey=OAISCAWXQQWLIC-NTYYTJCMSA-N

InChI=1S/C60H74N12O10.C2H4O2/c1-37(73)54-59(81)70-50(31-39-18-6-3-7-19-39)60(82)72(36-51(62)74)29-15-26-52(75)63-28-14-25-53(76)66-47(30-38-16-4-2-5-17-38)56(78)68-49(33-41-35-65-45-23-11-9-21-43(41)45)58(80)69-48(32-40-34-64-44-22-10-8-20-42(40)44)57(79)67-46(55(77)71-54)24-12-13-27-61;1-2(3)4/h2-11,16-23,34-35,37,46-50,54,64-65,73H,12-15,24-33,36,61H2,1H3,(H2,62,74)(H,63,75)(H,66,76)(H,67,79)(H,68,78)(H,69,80)(H,70,81)(H,71,77);1H3,(H,3,4)/t37-,46+,47+,48-,49+,50+,54+;/m1./s1

HIDE SMILES / InChI

Molecular Formula	C60H74N12O10
Molecular Weight	1123.304
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	7 / 7
E/Z Centers	0
Optical Activity	UNSPECIFIED

Molecular Formula	C2H4O2
Molecular Weight	60.052
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24400774 | https://www.tvm-lifescience.com/aspireos-somatoprim-dg3173-program-acquired-by-cortendo-for-usd-30-million/ | https://www.biocompare.com/Life-Science-News/134187-Aspireo-Reports-Somatoprim-Phase-IIa-Proof-Of-Concept-Results-In-Acromegaly/

Somatoprim (DG3173) is a heptapeptide somatostatin analog (SSA) that binds with high affinity to sstr2, sstr4 and sstr5 and shows a very low insulin suppression in contrast to other SSA. Initially developed by Ipsen, it is under active development by licensee Aspireo Pharmaceuticals, an Israeli company. In vitro as well as in vivo testing showed a dose-dependent GH lowering effect. Somatoprim has demonstrated a unique receptor binding and pharmacological profile which is differentiated from SSAs that are currently marketed or in clinical development. In particular, Somatoprim has shown an improved side effect profile with reduced adverse effects on the gastrointestinal tract and glucose metabolism. Furthermore, assessment of growth hormone secretion in cultured human somatotroph adenoma tissue treated with Somatoprim indicates that it has the potential to increase the response rate of acromegalic patients to SSA therapy. Somatoprim is currently in phase I/II of clinical development.

Originator

Approval Year

PubMed

Title	Date	PubMed
Pharmacotherapy: Somatoprim versus octreotide in acromegaly.	2011 Nov 29	22124440
A transplantable phosphorylation probe for direct assessment of G protein-coupled receptor activation.	2012	22745760
Emerging drugs for acromegaly.	2014 Mar	24400774
[Current and future therapy of acromegaly].	2016 Fall	27734694

Sample Use Guides

In Vivo Use Guide

Acromegaly: octreotide and Somatoprim (DG3173). Eligible patients are to receive 300 ug octreotide as active comparator, followed by four ascending doses of 100 ug, 300 ug, 900 ug and 1800 ug DG3173. All treatments will be administered consecutively to all patients as single subcutaneous bolus injections.

Route of Administration: Other

In Vitro Use Guide

PTR-3173 suppressed GH release from both fetal pituitaries (maximal suppression of 54% with 10 nM) and cultures of GH-cell adenomas (35% suppression with 100 nM).

Substance Class	Chemical Created by `admin` on `Sat Dec 16 13:18:46 GMT 2023` Edited by `admin` on `Sat Dec 16 13:18:46 GMT 2023`
Record UNII	9F2286627L
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

VELDOREOTIDE ACETATE

Common Name

English

SOMATOPRIM ACETATE

Common Name

English

COR-005 ACETATE

Code

English

Classification Tree Code System Code

FDA ORPHAN DRUG

397713

Created by admin on Sat Dec 16 13:18:46 GMT 2023 , Edited by admin on Sat Dec 16 13:18:46 GMT 2023

EU-Orphan Drug

EU/3/12/1075

Created by admin on Sat Dec 16 13:18:46 GMT 2023 , Edited by admin on Sat Dec 16 13:18:46 GMT 2023

Code System Code Type Description

FDA UNII

9F2286627L

Created by admin on Sat Dec 16 13:18:46 GMT 2023 , Edited by admin on Sat Dec 16 13:18:46 GMT 2023

PRIMARY

PUBCHEM

131634006

Created by admin on Sat Dec 16 13:18:46 GMT 2023 , Edited by admin on Sat Dec 16 13:18:46 GMT 2023

PRIMARY

Related Record Type Details


					1Z83587HBN

VELDOREOTIDE

PARENT -> SALT/SOLVATE

Related Record Type Details


					1Z83587HBN

VELDOREOTIDE

ACTIVE MOIETY