histrelin

Trade name: supprelin

Small moleculeapprovedOrphan Drug ^FDA

Approved

Dec 24, 1991

Histrelin is a gonadotropin releasing hormone (GnRH) agonist that acts as a potent inhibitor of gonadotropin when administered as an implant that delivers continuous therapeutic doses. Following an initial stimulatory phase with increased circulating levels of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to a transient increase in concentration of gonadal steroids (testosterone and dihydrotestosterone in males), continuous administration of histrelin acetate results in decreased levels of LH and FSH due to a reversible down-regulation of the GnRH receptors in the pituitary gland and desensitization of the pituitary gonadotropes. As the product Supprelin LA (FDA), histrelin is indicated for the treatment of children with central precocious puberty (CPP). As the product Vantas (FDA), histrelin is indicated for the palliative treatment of advanced prostate cancer. — NCATS

Clinical trial activity

10 trials · 9 clinical orgs · 4 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Apr 1, 2000 (NCT01697384)

Timeline

1980s

Aug 10, 1988
Orphan Drug Designation

1990s

Dec 24, 1991
Earliest FDA Approval
Dec 24, 1991
Shire — NDA Secondary Org
Dec 28, 1991
Johnson and Johnson — First NDA Organization
Dec 28, 1991
Johnson and Johnson — NDA Organization

2000s

Jan 1, 2000
Endo Pharmaceuticals — Earliest Phase 3 Sponsor(trial)
Oct 12, 2004
Endo Pharmaceuticals — NDA Secondary Org
Oct 12, 2004
Endo Pharmaceuticals — Marketing Organization
Oct 12, 2004
Bristol-Myers Squibb — NDA Secondary Org

2010s

Jan 1, 2015
Earliest Phase 2 Sponsor(trial)
Jan 1, 2019
Earliest Phase 1 Sponsor(trial)

Indications

Approved for

Prostatic Neoplasms (approved 2004)

Studied for

Mechanism of action

Gonadotropin-releasing hormone receptorAGONIST
GNRHR agonist
- Gonadotropin-releasing hormone receptor (GNRHR) ↗

Approval history

approvedPriority reviewDec 24, 1991

Chemistry & pharmacology

Loading structure…

SMILES

CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1cn(Cc2ccccc2)cn1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1

Mol. weight: 1323.53 g/mol
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No
Delivery: Parenteral
Availability: Prescription Only

Oral

Parenteral

Yes

Topical

Sources

Also known as

5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-1-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-1-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-nτ-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide
5-oxo-l-prolyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-nτ-benzyl-d-histidyl-l-leucyl-l-arginyl-n-ethyl-l-prolinamide
6-his(imbzl)-9-n-et-pronh2-10-des-glynh2-lhrh
gnrh, his(imbzl)(6)-n-et-pronh2(9)-
histrelin
histrelin
histrelin
histrelin
histrelin
histrelin
histrelin
histrelin
histrelina
histrelina
histrelin acetate
histrelin acetate
histrelin acetate
histrelin acetate
histrelin acetate
histrelin acetate
histreline
histreline
histrelinum
histrelinum
ibhpe-lhrh
[(im-bzl)-d-his6,pro9-net]-gonadotropin releasing hormone
[(im-bzl)-d-his6,pro9-net]-gonadotropin releasing hormone
((im bzl)-d-his(6), pro(9)-net)lhrh
imbzl-his(6), pro(9)-net-gnrh
lhrh, his(imbzl)(6)-n-et-pronh2(9)-
lhrh, histidyl(imbzl)(6)-n-ethylprolinamide(9)-des-glycinamide(10)-
l-pyroglutamyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-nim-benzyl-histidyl-l-leucyl-l-arginyl-l-proline ethylamide
l-pyroglutamyl-l-histidyl-l-tryptophyl-l-seryl-l-tyrosyl-d-nim-benzyl-histidyl-l-leucyl-l-arginyl-l-proline ethylamide
luteinizing hormone-releasing factor, 6-(1-(phenylmethyl)-d-histidine)-9-(n-ethyl-l-prolinamide)-10-deglycinamide-
luteinizing hormone-releasing factor (pig)
orf-17070
orf-17070
rwj-17070
rwj-17070
supprelin
supprelin
supprelin
supprelin
supprelin la
supprelin la
vantas
vantas
vantas
vantas
vantas

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT06378866	Phase 2	Jun 3, 2024	Mayo Clinic
NCT05050084	Phase 3	Nov 11, 2021	National Cancer Institute (NCI), NRG Oncology
NCT04787744	Phase 2/Phase 3 (Phase 3)	Jul 1, 2021	Department of Veteran Affairs
NCT04513717	Phase 3	Dec 15, 2020	National Cancer Institute (NCI), NRG Oncology
NCT03948828	Phase 1	Jun 1, 2019	Shenzhen University
NCT03678025	Phase 3	Sep 17, 2018	National Cancer Institute (NCI), Southwest Oncology Group
NCT02278185	Phase 2	Nov 11, 2015	University of Colorado, Denver
NCT00779103	Phase 3	Sep 1, 2004	Endo Pharmaceuticals, Indiana University
NCT01394263	Phase 3	May 1, 2000	Endo Pharmaceuticals
NCT01697384	Phase 3	Apr 1, 2000	Endo Pharmaceuticals

Showing 10 of 10 trials

Page 1 / 1

Organizations

Research & Development (9)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Endo Pharmaceuticals	For profit	3	3	1	2000
National Cancer Institute (NCI)	Government	3	0	1	2018
NRG Oncology	Academic/Hospital	2	2	1	2020
Department of Veteran Affairs	Government	1	1	1	2021
Indiana University	Academic/Hospital	1	0	1	2004
Mayo Clinic	Academic/Hospital	1	1	1	2024
Shenzhen University	Academic/Hospital	1	1	1	2019
Southwest Oncology Group	Academic/Hospital	1	1	1	2018
University of Colorado, Denver	Academic/Hospital	1	1	1	2015

9 organizations

Page 1 / 1

Marketing (5)

Organization	Org type	Relationship	Date
Bristol-Myers Squibb	For profit	NDA2	Oct 12, 2004
Endo Pharmaceuticals	For profit	NDA2	Oct 12, 2004
Endo Pharmaceuticals	For profit	MKTG	Oct 12, 2004
Johnson and Johnson	For profit	NDA	Dec 28, 1991
Shire	For profit	NDA2	Dec 24, 1991