VELDOREOTIDE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C60H74N12O10
Molecular Weight	1123.304
Optical Activity	UNSPECIFIED
Defined Stereocenters	7 / 7
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[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=ABFNTRQPWNXUHA-VEVJRHMJSA-N

InChI=1S/C60H74N12O10/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/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)/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

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
[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 01:54:33 UTC 2023` Edited by `admin` on `Sat Dec 16 01:54:33 UTC 2023`
Record UNII	1Z83587HBN
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

VELDOREOTIDE

Official Name

English

veldoreotide [INN]

Common Name

English

COR-005

Code

English

N4.1-(2-AMINO-2-OXOETHYL)-CYCLO(4-AMINOBUTANOYL-4-AMINOBUTANOYL-L-PHENYLALANYL-L-TRYPTOPHYL-D-TRYPTOPHYL-L-LYSYL-L-THREONYL-L-PHENYLALANYL)

Systematic Name

English

GLYCINAMIDE, N-(4-AMINO-1-OXOBUTYL)-L-PHENYLALANYL-L-TRYPTOPHYL-D-TRYPTOPHYL-L-LYSYL-L-THREONYL-L-PHENYLALANYL-N2-(3-CARBOXYPROPYL)-, (7->1)-LACTAM

Common Name

English

PTR-3173

Code

English

Veldoreotide [WHO-DD]

Common Name

English

VELDOREOTIDE [USAN]

Common Name

English

DG3173

Code

English

SOMATOPRIM

Common Name

English

DG-3173

Code

English

PTR 3173

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C62799