RPEP-00849 · 2003PT-141 (bremelanotide) induced sexual arousal in both male and female animals through central MC3R/MC4R activation, representing a mechanistically novel approach to sexual dysfunction treatment through brain desire pathways rather than peripheral blood flow.
Molinoff, P B; Shadiack, A M; Earle, D; Diamond, L E; Quon, C Y · Animal Study
RPEP-00903 · 2004Intranasal PT-141 induced dose-dependent erectile responses in both healthy men and Viagra-responsive ED patients in a double-blind, placebo-controlled trial, with rapid onset and acceptable safety — validating intranasal melanocortin ED therapy.
Diamond, L E; Earle, D C; Rosen, R C; Willett, M S; Molinoff, P B · RCT
RPEP-00924 · 2004PT-141 intranasal demonstrated ED treatment efficacy in clinical trials through central melanocortin receptor activation, with development progressing toward potential approval as a first-in-class brain-acting sexual dysfunction therapy.
Hedlund, Petter · Review
RPEP-00959 · 2004PT-141 (melanocortin agonist) selectively increased sexual solicitation (proceptive) behavior in female rats without affecting locomotion or other behaviors — demonstrating specific melanocortin modulation of female sexual desire/motivation.
Pfaus, James G; Shadiack, Annette; Van Soest, Tanya; Tse, Maric; Molinoff, Perry · Animal Study
RPEP-00969 · 2004SC PT-141 induced dose-dependent erectile responses in ED patients (double-blind, placebo-controlled) with characterized pharmacokinetics, acceptable safety, and practical SC delivery — advancing toward clinical approval.
Rosen, R C; Diamond, L E; Earle, D C; Shadiack, A M; Molinoff, P B · RCT
RPEP-01028 · 2005Co-administration of low-dose intranasal PT-141 (melanocortin agonist) with sildenafil (PDE5 inhibitor) produced synergistic erectile responses in ED patients — combining central desire/arousal with peripheral vasodilation for superior outcomes.
Diamond, L E; Earle, D C; Garcia, W D; Spana, C · RCT
RPEP-01128 · 2006Intranasal bremelanotide (PT-141) significantly increased subjective sexual arousal, desire, and genital sensation in premenopausal women with sexual arousal disorder in a double-blind, placebo-controlled RCT — landmark evidence leading toward FDA approval for female sexual dysfunction.
Diamond, Lisa E; Earle, Dennis C; Heiman, Julia R; Rosen, Raymond C; Perelman, Michael A; Harning, Ronald · RCT
RPEP-01279 · 2007Bremelanotide activates female sexual function through MC3R/MC4R in hypothalamic/limbic sexual circuits, enhancing desire and arousal through dopaminergic and oxytocinergic pathway modulation — the comprehensive CNS mechanism supporting its clinical development for female HSDD.
Pfaus, James; Giuliano, François; Gelez, Hélène · Review
RPEP-01288 · 2007Melanocortin agonists (bremelanotide, melanotan II) treat sexual dysfunction in both sexes through central MC3R/MC4R activation: ED in men and HSDD/FSAD in women — the only drug class targeting desire/arousal centrally for both genders.
Shadiack, Annette M; Sharma, Shubh D; Earle, Dennis C; Spana, Carl; Hallam, Trevor J · Review
RPEP-01346 · 2008Novel macrocyclic melanocortin peptides synthesized by microwave-assisted methods showed potent MC1R/MC4R activity, with the macrocyclic constraint improving receptor selectivity and metabolic stability — advancing circular peptide drugs for melanocortin receptor-mediated therapies.
Grieco, Paolo; Cai, Minying; Liu, Lu; Mayorov, Alexander; Chandler, Kevin; Trivedi, Dev; Lin, Guangxin; Campiglia, Pietro; Novellino, Ettore; Hruby, Victor J · In Vitro
RPEP-01413 · 2008SC bremelanotide significantly improved erectile responses in sildenafil-failure ED patients in a double-blind, placebo-controlled RCT — demonstrating melanocortin central mechanism (desire/arousal) rescues patients where PDE5 peripheral mechanism (blood flow) fails.
Safarinejad, Mohammad Reza; Hosseini, Seyyed Yousof · RCT
RPEP-04991 · 2020Bremelanotide significantly improved desire and reduced HSDD-related distress in Phase 2/3 trials, with nausea (39.9%), flushing (20.4%), and headache (11%) as main side effects.
Mayer, Danielle; Lynch, Sarah E · Review
RPEP-05507 · 2021From 242 exit surveys and 80 telephone interviews, bremelanotide-treated women described increased sexual desire, physical arousal, and improved sexual activity quality — physiological responses not reported by placebo-treated women, who described non-physiological benefits only.
Koochaki, Patricia; Revicki, Dennis; Wilson, Hilary; Pokrzywinski, Robin; Jordan, Robert; Lucas, Johna; Williams, Laura A; Sadiq, Amama; Krop, Julie · Rct