Vyleesi (bremelanotide) / Kwang Dong, Fosun Pharma, Palatin Technologies - LARVOL DELTA

The Rise of Peptide Therapies and Anesthetic Risk: A Case Report Emphasizing Preoperative Medication Disclosure (ASA 2026) - "Peptide therapies including GLP-1 agonists (aspiration risk from delayed gastric emptying), BPC-157 (unapproved, potential local anesthetic interactions), melanotan 1/2 (cardiovascular effects), and PT-141/bremelanotide (cardiovascular effects) are increasingly used but rarely disclosed by patients. These substances, often obtained through unregulated sources, carry significant anesthetic risks including aspiration, hemodynamic instability, and drug interactions. Systematic preoperative screening with direct questioning about weight loss medications, supplements, and wellness peptides is essential for patient safety."

Case report • Clinical • Cardiovascular • Gastroenterology

Comprehensive characterization of bremelanotide acetate and its degradants by LC-HRMS/MS and predicting epimerization through computational modelling. (PubMed, Anal Methods) - "ProTox-3.0-based in silico toxicity prediction indicated that most degradation products belonged to toxicity class 5, while two hydrolytic products were classified as class 4. Overall, this study provides valuable insights into BRM stability behavior and supports peptide API/formulation development, impurity profiling, and quality control."

Journal

Goldilocks-Inspired Design of Mid-Size Macrocycles for Selective Targeting of Human Melanocortin Receptors. (PubMed, J Med Chem) - "The recent clinical success of macrocyclic peptides, such as bremelanotide and setmelanotide, highlights the potential of this modality as a "Goldilocks" chemical class, effectively balancing the properties of small molecules and biologics while optimizing their affinity, stability, and pharmacokinetics. Additionally, FM635 exhibited interesting agonist activity with remarkable selectivity for the same receptor. This study underscores the potential of tailored midsized macrocycles as selective MCR ligands and provides new insights into the structure-activity relationships, thereby guiding the development of therapeutic candidates for metabolic and inflammatory diseases."

Journal • Inflammation • MC4R

The Investigation of Bremelanotide'S Role in Modulating Sexual Function and Repetitive Behaviors in Mice. (ENDO 2026) - "Bremelanotide induces a dramatic increase in grooming behavior that correlates with dosage. Here, we demonstrate that bremelanotide primarily acts through melanocortin receptors on vasopressin neurons to facilitate grooming phenotypes by inducing a knockout of the receptor on the target neurons and subsequently testing grooming phenotypes."

Preclinical • Sexual Disorders • MC4R

Clinical trial evidence on emerging pharmacological therapies for hypoactive sexual desire disorder in women: a systematic review and analysis of completed studies registered on ClinicalTrials.gov. (PubMed, Front Med (Lausanne)) - "Investigational therapies predominantly targeted central nervous system pathways, with flibanserin and bremelanotide representing the most extensively studied agents. Variability in trial design, outcome measures, and reporting practices limits cross-trial comparison and clinical interpretation. Further research with standardized methodologies and comprehensive reporting is needed to strengthen the evidence base."

Clinical • Journal • Review • Sexual Disorders • Women's Health

Quantification of "Mercy Sex" in Heterosexual Women. (PubMed, J Sex Marital Ther) - "However, HSDD clinical trials evaluating testosterone therapy, flibanserin, and bremelanotide spanning nearly a decade show women with HSDD, encompassing low to no sexual desire, are still engaging in sexual activity. These results have important implications for further HSDD clinical research, as mercy sex frequency may skew therapeutic efficacy while having significant implications in calculating trial sample size, and assessing a clinically meaningful response to therapy, when SSEs are used as a primary endpoint. Although this paper explores only a biopsychosocial explanation for the phenomenon of mercy sex in clinical trials of HSDD therapies, it provides a valuable understanding that will benefit patients, clinicians, and researchers."

Journal • Review • Sexual Disorders

FDA-Approved Drugs Containing D-Amino Acids: A Historical and Developmental Perspective. (PubMed, Drug Dev Res) - "These drugs include both natural products like gramicidin D and synthetic analogs such as desmopressin, leuprolide, bremelanotide, and etelcalcetide, the latter being the first fully d-amino acid peptide to receive FDA approval. This review traces the historical development and clinical adoption of d-amino acid-containing drugs, highlighting their mechanisms of action, therapeutic relevance across disease areas, and the technological innovations, particularly solid-phase peptide synthesis and conceptual advances such as mirror-image phage display, that enabled their advancement. As peptide therapeutics continue to evolve, d-amino acids-containing drugs are poised to play a central role in the next generation of targeted, stable, and high-precision pharmaceuticals."

FDA event • Journal • Review • Endocrine Disorders • Infectious Disease

Therapeutic peptides in gerontology: mechanisms and applications for healthy aging. (PubMed, Front Aging) - "Search terms included "peptide therapeutics," "aging," "gerontology," "healthspan," combined with specific peptide names (tirzepatide, epitalon, GHK-Cu, BPC-157, TB-500, Semax, CJC-1295, ipamorelin, bremelanotide). Therapeutic peptides offer mechanistically diverse approaches to multiple aging hallmarks. While FDA-approved agents demonstrate clinical potential, investigational peptides require rigorous validation through well-designed clinical trials to establish safety and efficacy for healthspan extension."

Journal • Review • Metabolic Disorders

Should Bremelanotide Be Considered for the Treatment of Sexual Arousal and Desire Disorders in Men? (PubMed, J Clin Psychopharmacol) - No abstract available

Journal

Single Dose of Vyleesi in Lactating Female Subjects to Measure the Concentration of Bremelanotide in Breast Milk (clinicaltrials.gov) - P4 | N=10 | Completed | Sponsor: Cosette Pharmaceuticals, Inc. | Recruiting ➔ Completed

Trial completion

Strategies for Treating Sexual Health Concerns After Breast and Gynecologic Cancer. (PubMed, J Minim Invasive Gynecol) - "Sexual dysfunction following breast and gynecologic cancer requires individualized, multimodal management. A combination of non-hormonal and hormonal therapies, behavioral interventions, and emerging pharmacologic treatments offers promising avenues for improving sexual health and overall quality of life in survivors. Future research should focus on the effects of specific cancer therapies on sexual health, investigate the role of biological markers and dysfunction, and refine more personalized approaches to care."

Journal • Breast Cancer • Gynecologic Cancers • Oncology • Sexual Disorders • Solid Tumor • Women's Health

Co-Administration of Bremelanotide with Tirzepatide in Participants with Obesity (OBESITY WEEK 2025) - "In this controlled study, adding a low-dose MC4R agonist to low-dose tirzepatide resulted in greater weight loss over low-dose tirzepatide alone. The results are supportive of a potential positive, synergistic effect between these 2 mechanisms. Combined treatment was well tolerated, and there was no increase in GI AEs."

Genetic Disorders • Obesity • MC4R

Poster #2: Co-Administration of MC4R Agonist and Tirzepatide in Obese Patients (PRNewswire) - "Key findings include: Adding a low dose of an MC4R agonist led to greater weight loss compared to tirzepatide alone; No new safety concerns were observed; the combination was well tolerated, with no increase in gastrointestinal side effects; Sustained weight maintenance was seen, as low-dose MC4R activation helped prevent weight regain after stopping tirzepatide treatment."

P2 data • Obesity

Practical considerations and emerging approaches for the management of vasomotor and sexual symptoms in breast cancer patients on endocrine therapies. (PubMed, Expert Rev Clin Pharmacol) - "Pharmacologic therapy for VMS has been centered on selective serotonin reuptake inhibitors and serotonin norepinephrine reuptake inhibitors, gabapentin, and clonidine...This review summarizes the current pharmacologic therapy for VMS, focusing on the practical considerations for use of the novel VMS (fezolinetant, elinzanetant) and libido agents (flibanserin, bremelanotide)...These novel agents are eagerly awaited therapeutic options; however, clinical trials excluded breast cancer patients. This review provides clinicians with relevant considerations to assess when recommending these therapies for patients with breast cancer, while awaiting ongoing research to give additional insights for best tailoring therapy for this patient population."

Journal • Review • Breast Cancer • Oncology • Solid Tumor

Polymorphism of Melanocortin Receptor Genes-Association with Inflammatory Traits and Diseases. (PubMed, Diseases) - "Among them, α-MSH analogs play a role in atopic dermatitis and scleroderma, and MC1R agonist Dersimelagon has shown effectiveness in systemic sclerosis. The FDA has recently approved the repository corticotropin injection (RCI) to treat sarcoidosis. The FDA has also approved various melanocortin agonists, i.e., Bremelanotide, Afamelanotide, and Setmelanotide, for the treatment of hypoactive sexual desire disorder, Erythropoietic protoporphyria, and obesity, due to pro-opiomelanocortin and leptin receptor deficiency, respectively. Therefore, this review aims to summarize the function and genetic polymorphism of melanocortin receptors, regulatory pathways involving MCRs, and the existing evidence of the prime effect of MCRs on inflammatory responses via different mechanisms and their potential therapeutic use in inflammatory diseases."

Journal • Review • Alzheimer's Disease • Amyotrophic Lateral Sclerosis • Atopic Dermatitis • CNS Disorders • Depression • Dermatitis • Dermatology • Diabetes • Gastroenterology • Gastrointestinal Disorder • Genetic Disorders • Immunology • Inflammation • Inflammatory Bowel Disease • Major Depressive Disorder • Melanoma • Metabolic Disorders • Multiple Sclerosis • Obesity • Ocular Inflammation • Oncology • Ophthalmology • POMC-null Obesity • Psychiatry • Reperfusion Injury • Respiratory Diseases • Rheumatology • Sarcoidosis • Scleroderma • Sexual Disorders • Solid Tumor • Systemic Sclerosis • Type 2 Diabetes Mellitus • Uveitis • LEP • LEPR

Single Dose of Vyleesi in Lactating Female Subjects to Measure the Concentration of Bremelanotide in Breast Milk (clinicaltrials.gov) - P4 | N=10 | Recruiting | Sponsor: Cosette Pharmaceuticals, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open

FDA-approved drugs as potential covalent inhibitors of key SARS-CoV-2 proteins: an in silico approach. (PubMed, Turk J Biol) - "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."

FDA event • Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

2024 SOGC, 2024 NCCN, 2022 ESO, AND 2018 ASCO: A COMPARISON OF BREAST CANCER/SURVIVORSHIP GUIDELINES FOR THE MANAGEMENT OF SEXUAL HEALTH CONCERNS (MASCC-ISOO 2025) - "Although all guidelines, except ESO–ESMO, include recommendations for androgens, bupropion, flibanserin, bremelanotide, and buspirone for low sex drive, there is limited data to support the use of these interventions. Conclusions There is consensus between guidelines on sexual health recommendations, with some variation. Additional research is needed on pharmacological interventions and type of counselling to strengthen the evidence supporting these recommendations."

HEOR • Breast Cancer • Infectious Disease • Obstetrics • Oncology • Pain • Sexual Disorders • Solid Tumor

Title: Female Sexual Desire, Arousal, and Orgasmic Dysfunctions: A Systematic Review and Meta-analysis of Treatment Options. (PubMed, J Minim Invasive Gynecol) - "In this systematic review of treatments of females with sexual DAO dysfunctions without pain, we found that CBT improves DAO; flibanserin improves desire; and bremelanotide improves both desire and arousal; and all three treatments reduce distress. Our findings align with previous literature and expand upon it to include multiple treatment modalities. This broader perspective offers a starting point for clinicians, including gynecologists, who frequently serve as the first point of care for female sexual dysfunction. Conclusions regarding most other treatments could not be drawn due to limited numbers of studies of FSD excluding pain, heterogeneous terminology for DAO disorders, and varying outcome measures across studies."

Journal • Retrospective data • Pain • Sexual Disorders

2024 SOGC, 2024 NCCN, 2022 ESO-ESMO, and 2018 ASCO: a comparison of female cancer survivorship guidelines for the management of sexual health concerns. (PubMed, Support Care Cancer) - "There is consensus among guidelines on certain sexual health recommendations, with some variation. Additional research is needed on pharmacological interventions and types of counselling to strengthen their evidence."

Clinical • HEOR • Journal • Review • Infectious Disease • Obstetrics • Oncology • Pain • Sexual Disorders

A biodegradable suction patch for sustainable transbuccal peptide delivery. (PubMed, J Control Release) - "Recent studies on a bioinspired suction patch demonstrated positive effects in vivo with three peptides - desmopressin, semaglutide, and teriparatide - yet materials used for patch fabrication were non-degradable. Additionally, the patch achieved a relative bioavailability of 26 % for bremelanotide (1.03 kDa) compared to subcutaneous administration. This work underscores the potential of replacing silicone devices with biodegradable alternatives, providing a more sustainable approach for peptide delivery via the buccal suction patch."

Journal

Obesity Program Highlights (PRNewswire) - P2 | N=108 | NCT06565611 | Sponsor: Palatin Technologies, Inc | "Phase 2 Study Co-administration of Bremelanotide (MC4R agonist) + Tirzepatide (GLP-1/GIP dual agonist): Met primary endpoint in the 8-week treatment study with high statistical significance (p<0.0001). Patients receiving co-administration showed a 4.4% weight reduction, vs. 1.6% for placebo. 19% of patients achieved ≥7% weight loss (p<0.1). Low-dose bremelanotide prevented weight regain typically seen following tirzepatide discontinuation. No added tolerability or safety issues observed with the combination. IND filings planned for Q1 2026; initial clinical data expected in 1H 2026. Planned Phase 1 SAD/MAD studies will include patients with hypothalamic obesity."

IND • New P1 trial • P2 data • Obesity

Palatin Reports Positive Appetite Suppression Results From Phase 2 Obesity Study of MC4R Agonist Bremelanotide and Tirzepatide (PRNewswire) - P2 | N=108 | NCT06565611 | Sponsor: Palatin Technologies, Inc | "Palatin Technologies, Inc...announced positive appetite suppression results from its BMT-801 Phase 2 obesity study. The study included a co-administered melanocortin 4 receptor (MC4R) agonist bremelanotide plus glucagon like peptide-1/gastric inhibitory polypeptide (GLP-1/GIP) tirzepatide arm, bremelanotide alone, and tirzepatide alone arms...Overall appetite suppression: Bremelanotide + tirzepatide: 71% increase; Tirzepatide only: 73% increase; Bremelanotide only: 71% increase...'How full do you feel (fullness)?': Bremelanotide + tirzepatide: 65% increase; Tirzepatide only: 62% increase; Bremelanotide only: 79% increase...'How satisfied do you feel (satiety)?': Bremelanotide + tirzepatide: 56% increase; Tirzepatide only: 56% increase; Bremelanotide only: 68% increase."

P2 data • Patient reported outcomes • Obesity

Oxytocin for male orgasmic disorder: fact or fiction? (AUA 2025) - "This starts with vibratory stimulation, followed by oxytocin, bupropion, and cabergoline, and finally bremelanotide and flibanserin. Intranasal oxytocin failed to significantly improve orgasmic disorder in the majority of men in our cohort. Male orgasmic disorder remains a difficult to treat condition. A significant proportion of patients with orgasmic disorder are co-morbid with erectile dysfunction and a psychiatric diagnosis, most commonly major depressive disorder."

CNS Disorders • Depression • Endocrine Disorders • Erectile Dysfunction • Major Depressive Disorder • Mental Retardation • Mood Disorders • Psychiatry • Sexual Disorders

Palatin to Present Positive Phase 2b Data for Melanocortin Agonist in Diabetic Kidney Disease at the National Kidney Foundation Spring Meeting (PRNewswire) - P2b | N=16 | BREAKOUT (NCT05709444) | Sponsor: Palatin Technologies, Inc | "Palatin Technologies...today announced that data from the Phase 2b BREAKOUT study will be presented today at the National Kidney Foundation Spring Meeting in Boston, MA. The poster presentation titled Efficacy of Bremelanotide (BMT) to Stabilize Podocyte Function and Reduce Proteinuria in Adults with Diabetic Type II Nephropathy...71% of patients achieved a >30% reduction in the urine protein to creatinine ratio (UP/Cr), a key indicator of kidney damage. 71% of patients demonstrated improved or stabilized estimated glomerular filtration rate (eGFR), signaling preserved kidney function. 37.5% of patients had increased urinary vascular endothelial growth factor (VEGF) levels, suggesting better blood vessel support in the kidneys. 36% of patients had reduced urinary synaptopodin loss, indicating healthier kidney cells and structure."

P2b data • Diabetic Nephropathy • Renal Disease