abarelix

Trade name: plenaxis

Small moleculeapproved

Approved

Nov 25, 2003

Abarelix is a synthetic decapeptide antagonist to gonadotropin releasing hormone (GnRH). It is marketed by Praecis Pharmaceuticals as Plenaxis. Used in the palliative treatment of advanced prostate cancer. Abarelix is a luteinizing hormone agonist that results in suppression of testicular or follicular steroidogenesis. Abarelix binds to the gonadotropin releasing hormone receptor and acts as a a potent inhibitor of gonadotropin secretion. Praecis announced in June 2006 that it was voluntarily withdrawing the drug from the market. — NCATS

Clinical trial activity

3 trials · 3 clinical orgs · 2 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Jan 1, 1999 (NCT00841113)

Timeline

1990s

Jan 1, 1999
Contura — Earliest Phase 3 Sponsor(trial)

2000s

Nov 25, 2003
Earliest FDA Approval
Nov 25, 2003
Contura — NDA Secondary Org
Jan 1, 2004
Praecis Pharmaceuticals — Earliest Phase 2 Sponsor(trial)

Indications

Approved for

Prostatic Neoplasms (approved 2003)

Studied for

Prostatic Neoplasms · Phase 4

Mechanism of action

Gonadotropin-releasing hormone receptorANTAGONIST
GNRHR antagonist
- Gonadotropin-releasing hormone receptor (GNRHR) ↗

Approval history

approvedPriority reviewNov 25, 2003

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)C[C@H](NN[C@H](CC(N)=O)C(=O)C(=O)[C@H](CC1=CC=C(O)C=C1)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](CC2=CN=CC=C2)NC(=O)[C@@H](CC3=CC=C(Cl)C=C3)NC(=O)[C@@H](CC4=CC5=C(C=CC=C5)C=C4)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N6CCC[C@H]6C(=O)N[C@H](C)C(N)=O

Mol. weight: 1416.063 g/mol
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Parenteral
Availability: Discontinued

Oral

Parenteral

Yes

Topical

Black box warning

Sources

Also known as

abarelix
abarelix
abarelix
abarelix
abarelix
abarelix
abarelix
abarelix
abarelix
abarelix
abarelix
abarelix
n-acetyl-3-(2-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-n-methyl-l-tyrosyl-d-asparaginyl-l-leucyl-n(6)-(1-methylethyl)-l-lysyl-l-prolyl-d-alaninamide
plenaxis
plenaxis
plenaxis
plenaxis
plenaxis
ppi-149
ppi-149
ppi-149
ppi-149
r3827
r-3827
r-3827

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT00103623	Phase 4	Jun 1, 2004	Praecis Pharmaceuticals
NCT00100243	Phase 2	May 1, 2004	Praecis Pharmaceuticals
NCT00841113	Phase 3	Jan 1, 1999	Contura, Radboud University

Showing 3 of 3 trials

Page 1 / 1

Organizations

Research & Development (3)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Praecis Pharmaceuticals	For profit	2	2	2	2004
Contura	For profit	1	1	1	1999
Radboud University	Academic/Hospital	1	0	1	1999

3 organizations

Page 1 / 1

Marketing (2)

Organization	Org type	Relationship	Date
Contura	For profit	NDA2	Nov 25, 2003
Praecis Pharmaceuticals	For profit	NDA	—