Drug Database
HI

histrelin (histrelin implant / RL0903 / VP001)

✓ Approved

BioPro Pharmaceutical, Inc. · GNRHR · Small Molecule

What is histrelin?

histrelin is a small molecule developed by BioPro Pharmaceutical, Inc.. It is approved for therapeutic indications via injectable (others) or subcutaneous injection or surgical implantation.

Drug Profile

Brand Nameshistrelin implant, RL0903, VP001
CompanyBioPro Pharmaceutical, Inc.
Drug ClassSmall Molecule, Polypeptide
Molecular TargetGNRHR
RouteInjectable (Others), Subcutaneous Injection, Surgical Implantation
StatusApproved
Sources: ClinicalTrials.gov, BioPro Pharmaceutical, Inc.

Mechanism of Action

Molecular Targets

histrelin acts on 1 molecular target:

GNRHRgonadotropin releasing hormone receptor (HH7, GRHR)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

histrelin is developed for 2 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Prostate cancer✓ Approved
Psychiatric disordersDrug dependencePreclinical

Related Research Articles

PubMedFrontiers in endocrinology2026-10-24

Case Report: Sustained pubertal suppression for 68 months with a single histrelin acetate implant in central precocious puberty.

Ilmer Sofya S, Salemi Parissa P

The subcutaneous histrelin acetate implant is FDA-approved for 12 months of continuous gonadotropin-releasing hormone (GnRH) agonist therapy in central precocious puberty (CPP). Published data demonstrated sustained suppression with a single implant for up to approximately 24 months; however, efficacy beyond this duration has not been reported. A 7 years 5 month old female patient presented with bilateral Tanner 2 breast development, a bone age of 10 years, and laboratory findings consistent with early central activation. Treatment was delayed 11 months due to disruptions in care during the COVID-19 pandemic, and a histrelin implant was placed at age 8 years 5 months. The patient was lost to follow-up and returned at nearly 14 years of age, approximately 68 months after the implant placement, with primary amenorrhea and pubertal arrest. Laboratory evaluation before implant removal showed suppressed but detectable gonadotropins with a prepubertal estradiol, consistent with sustained partial suppression of the hypothalamic-pituitary-gonadal (HPG) axis sufficient to arrest pubertal progression. Her predicted adult height (PAH) of 167.6 cm (66 inches) approximated her mid-parental height (MPH) of 166.4 cm (65.5 inches). This case demonstrates that a single histrelin acetate implant may maintain clinically meaningful pubertal suppression for at least 68 months. These findings support broader investigations into the pharmacokinetics of extended implant use, given implications for reducing surgical burden and healthcare costs in CPP management.

PMID 42920604
Read full article →
PubMedVeterinary research communications2026-10-20

Low-dose histrelin for ovulation induction in mares: a partially randomized crossover pilot study.

de Barros Fogagnoli Lys L, Jose Kallena Canali Abdala KCA, Weckl Rachel R, Mota Clara Mantovani Ozorio CMO et al.

This partially randomized crossover pilot study evaluated reduced doses of histrelin for ovulation induction in mares and compared intramuscular (IM) administration with pharmacopuncture at the Bai-hui and Yan-chi acupoints. Eleven mares were enrolled, of which nine completed all eight protocols and were included in the analyses. The protocols comprised 250 µg histrelin IM (standard dose), 75 µg IM, 25 µg IM, no intervention, saline at Bai-hui, saline at Yan-chi, 25 µg histrelin at Bai-hui, and 25 µg histrelin at Yan-chi. Ovulation was assessed by transrectal ultrasonography at scheduled examinations until detected, with ovulation within 48 h as the primary outcome. Ovulations first detected at 24 h were excluded from the primary analysis. Ovulation within 48 h occurred in 88.9% (8/9) of observations with 250 µg IM, 87.5% (7/8) with 75 µg IM, 87.5% (7/8) with 25 µg IM, 37.5% (3/8) with no intervention, 50.0% (3/6) with saline at Bai-hui, 100% (9/9) with 25 µg histrelin at Bai-hui, 12.5% (1/8) with saline at Yan-chi, and 87.5% (7/8) with 25 µg histrelin at Yan-chi. Exact 95% confidence intervals were wide, reflecting the small sample size. Exploratory pairwise comparisons with the no-intervention protocol were performed without adjustment for multiple comparisons and should be interpreted cautiously. The findings provide preliminary evidence that reduced histrelin doses, including 25 µg, may induce ovulation within 48 h in mares. However, this study did not demonstrate an advantage of pharmacopuncture over IM administration of the same reduced dose. Larger, fully randomized studies are required to confirm the efficacy of reduced-dose histrelin and determine whether administration at specific acupoints provides any additional effect.

PMID 42897392
Read full article →
PubMedTurkish journal of biology = Turk biyoloji dergisi2025-07-18

FDA-approved drugs as potential covalent inhibitors of key SARS-CoV-2 proteins: an in silico approach.

Serilmez Murat M, Abuelrub Anwar A, Erol Ismail I, Durdaği Serdar S

The COVID-19 pandemic caused by SARS-CoV-2 necessitated rapid development of effective therapeutics, prompting this study to identify potential inhibitors targeting key viral and host proteins: RNA-dependent RNA polymerase (RdRp), main protease (Mpro), transmembrane serine protease 2 (TMPRSS2), and angiotensin-converting enzyme 2 (ACE2). We used covalent docking and molecular dynamics (MD) simulations to screen FDA-approved compounds against these targets using diverse covalent reaction mechanisms. Top-ranking compounds underwent further evaluation through MD simulations to assess binding stability and conformational dynamics. Several promising drug repurposing candidates were identified: bremelanotide, lanreotide, histrelin, and leuprolide as potential RdRp inhibitors; azlocillin, cefiderocol, and sultamicillin for Mpro inhibition; tenapanor, isavuconazonium, and ivosidenib targeting TMPRSS2; and cefiderocol, cefoperazone, and ceftolozane as potential ACE2 inhibitors. This study provides valuable insights into repurposing existing drugs as potential COVID-19 therapeutics by targeting crucial viral proteins. However, further experimental validation and preclinical studies are necessary to confirm the efficacy and safety of these compounds before consideration for clinical application.

PMID 40678415
Read full article →
PubMedPloS one2025-07-11

Adverse event profile differences among long-acting gonadotropin-releasing hormone analogs: A real-world, pharmacovigilance study.

Chen Yuting Y, Lu Weitao W, Liao Ruilian R, Zhang Ximin X et al.

Long-acting Gonadotropin-releasing hormone analogs(GnRHa), including leuprolide, goserelin, histrelin, buserelin, triptorelin, have been widely used for a variety of diseases including prostate cancer, breast cancer, endometriosis, uterine leiomyomas, and central precocious puberty (CPP). However, their real-world safety profile differences have not been adequately compared. We aimed to investigate the adverse event (AE) profile differences of long-acting GnRHa reported by the US Food and Drug Administration Adverse Event Reporting System (FAERS). All indications were searched long-acting GnRHa, as primary suspect drugs, from FAERS data (January 2004 to September 2023). We performed disproportionality analyses by reporting odds ratios (ROR) and conducted univariate and multivariate logistical regression analyses to determine the odds ratio (OR) of serious AEs associated with long-acting GnRHa under different exposure factors. Reproductive system and breast disorders accounted for the greatest proportion of adverse events among the five long-acting GnRHa formulations analyzed. Both buserelin and histrelin showed distinct adverse effect profiles, with buserelin demonstrating a higher incidence of gastrointestinal disorders and histrelin showing a greater propensity for psychiatric disorders. Logistic regression analysis revealed these five medications carried an elevated risk of significant medical events, and this risk was notably lower in pediatric patients (<18 years) compared to adult populations (≥18 years). Significant disparities exist between the adverse event profiles of long-acting GnRHa. The identification of high-risk factors and the enhancement of AEs monitoring are crucial during clinical application.

PMID 40644420
Read full article →
PubMedClinical therapeutics2025-05-10

The US Supreme Court Joins the Debate Over Gender Dysphoria.

Boumil Marcia M MM, Beninger Paul P

US v. Skrmetti is a legal case currently pending before the US Supreme Court that addresses the constitutionality of a Tennessee statute that prohibits gender-affirming medical care for transgender individuals who have not yet reached the legal age of adulthood, and who are diagnosed with gender dysphoria. Twenty-five other states have similar bans that apply to adolescents diagnosed with gender dysphoria, who are seeking treatment recommended by a physician and who are supported by their parents. Treatment involves gonadotropin-releasing hormone agonists, such as leuprolide or histrelin, which are approved by the Food and Drug Administration for use in children with central precocious puberty and are commonly prescribed off-label for adolescents. The purpose of puberty-blocking drugs is to suppress the onset of hormonal changes of puberty to facilitate the youth's anticipated transgender transition when the youth does reach the legal age of adulthood. Certainty about the time available for a youth to consider their gender identity, with the guidance of a professional support team, minimizes the risk of disruptive anxiety that's associated with near-term onset of sexual maturation involving development of irreversible secondary sex characteristics. This Commentary presents the legal arguments in the case and discusses relevant medical literature on this important issue in anticipation of the US Supreme Court's decision on the Tennessee law.

PMID 40345908
Read full article →
PubMedFuture oncology (London, England)2025-04-07

Study of persistence and adherence to ADT in prostate cancer: relugolix, degarelix, and GnRH agonists in the US.

Hafron Jason J, Hong Agnes A, Ryan Michael J MJ, Romdhani Hela H et al.

Androgen deprivation therapy (ADT) is standard for advanced prostate cancer. Relugolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, is the only oral ADT, with limited real-world data on therapy persistence and adherence. This retrospective study evaluates persistence and adherence of relugolix, degarelix, and GnRH agonists (leuprolide, goserelin, triptorelin, histrelin) using data from the IBM MarketScan Research Database (Jan 2017 - Dec 2022). The IBM MarketScan Research Database (1 January 2017 - 31 December 2022) was used for enrollment history and claims. ADT adherence was measured by the proportion of days covered (PDC) at 3, 6, and 12 months, calculated as days on ADT divided by period duration. Kaplan-Meier analysis assessed treatment persistence by measuring time to treatment discontinuation. Relugolix had higher adherence (PDC ≥ 80%) at 12 months (60.8%) compared to degarelix (13.0%) and GnRH agonists (46.3%). Median time to discontinuation was also longer for relugolix (13.5 months) than degarelix (3.1 months) and GnRH agonists (8.8 months). Persistence and adherence rates were higher in metastatic prostate cancer. Findings support relugolix use as an oral treatment due to its favorable persistence and long-term adherence profiles.

PMID 40189880
Read full article →

+87 more articles available with a free account

Sign up free to view all articles →

Ask about histrelin