1. Description
Treatment of Respiratory Diseases: Aviptadil is being developed as an injectable formulation and nebulized inhalation agent for the treatment of pulmonary arterial hypertension (PAH), acute respiratory distress syndrome (ARDS), and chronic obstructive pulmonary disease (COPD). Improves right ventricular function in PAH patients by dilating pulmonary vessels and reducing pulmonary vascular resistance; simultaneously suppresses release of pulmonary inflammatory mediators (TNF-α, IL-6) to mitigate tissue damage, enhance respiratory function, and serve patients intolerant to conventional vasodilators.
Cardiovascular Disease Adjunctive Therapy: Aviptadil is being developed as an adjunctive therapy for heart failure and coronary heart disease. It dilates coronary arteries to improve myocardial perfusion, alleviates myocardial ischemia and hypoxia, suppresses myocardial inflammatory responses, reduces myocardial fibrosis, and protects myocardial cell function. Suitable for long-term intervention in chronic heart failure patients.
Treatment for Erectile Dysfunction: Aviptadil is being developed as a local injection or gel formulation for erectile dysfunction (ED). By dilating penile cavernous vessels and increasing blood flow, it improves erection hardness and duration. It is particularly suitable for patients with vascular ED (e.g., diabetes- or hypertension-related ED) and has no contraindications for nitrates.
Inflammatory Bowel Disease Treatment: Aviptadil is being developed as an enema formulation or oral enteric-coated formulation for ulcerative colitis and Crohn's disease. By modulating intestinal mucosal immunity, suppressing intestinal inflammation, and promoting mucosal repair, it alleviates symptoms such as diarrhea, abdominal pain, and ulcers. It is suitable for patients with inflammatory bowel disease who are steroid-dependent or unresponsive to corticosteroids.
2. Application
Sensitive Skin & Inflammation Repair Products: Aviptadil targets rosacea, steroid-dependent dermatitis, and seasonal sensitivity, used in developing redness-relief serums and anti-inflammatory repair creams. Add at 0.01%-0.05% concentration. blended with Ceramide NP and Ectoin. By inhibiting the release of inflammatory mediators, it alleviates redness, dryness, itching, and stinging while strengthening the skin barrier, making it suitable for daily maintenance of fragile skin.
Medical Aesthetic Post-Treatment Repair Products: Aviptadil is suitable for use after procedures like photorejuvenation, laser treatments, and microneedling, for developing post-procedure soothing freeze-dried powders and repair serums. Formulation logic: Aviptadil (0.02%-0.03%) + Panthenol (2%-3%) + Asiaticoside (0.3%-0.5%) rapidly alleviates post-procedure redness and swelling, inhibits post-inflammatory hyperpigmentation, and accelerates damaged epidermal repair.
Scalp Anti-Inflammatory Care Products: Aviptadil targets individuals with seborrheic dermatitis, scalp itchiness, and dandruff (inflammation caused by Malassezia infection). Developed for anti-inflammatory shampoos and scalp repair serums. Addition concentration: 0.01%-0.03%. blended with tea tree oil and pyrithione zinc to suppress scalp inflammation, regulate the scalp microenvironment, reduce dandruff production, and relieve scalp itching.
3. Main Efficacy
Targeted Vasodilatory Effects: Aviptadil's core mechanism involves specifically binding to VPAC1 and VPAC2 receptors, activating adenylate cyclase (AC), elevating intracellular cAMP levels, relaxing vascular smooth muscle, and achieving vasodilation. — Highly selective for pulmonary vessels, coronary arteries, and penile cavernous bodies, reducing local vascular resistance and increasing tissue blood flow without systemic hypotension risk. Suitable for conditions involving vasospasm or hypoperfusion.
Potent anti-inflammatory and immunomodulatory effects: Aviptadil activates VPAC receptors to inhibit transcription and release of pro-inflammatory factors (TNF-α, IL-6, IL-1β) while upregulating anti-inflammatory factors (IL-10, TGF-β), thereby blocking inflammatory cascades. Additionally, it modulates immune cell (macrophage, T cell) activity, balances innate and adaptive immunity, and reduces tissue damage caused by excessive inflammation, providing relief for inflammation in multiple sites including lungs, intestines, and skin.
Tissue Repair and Mucosal Protection Effects: Promotes proliferation and differentiation of epithelial cells (respiratory tract, intestinal, and skin epidermal cells), accelerates repair of damaged mucosa/epidermis, and enhances tissue barrier integrity. — In the intestine, it promotes regeneration of intestinal mucosal epithelial cells and repairs ulcerated surfaces. In the skin, it promotes repair of stratum corneum cells, strengthens the skin barrier, and reduces transepidermal water loss. In the lungs, it protects airway epithelial cells and reduces mucosal damage caused by inflammation.
Safety Advantages: As a synthetic analog of endogenous VIP, Aviptadil exhibits exceptional biocompatibility, lacks immunogenicity, and does not trigger allergic or rejection reactions. Pharmaceutical-grade products have undergone acute/chronic toxicity testing, showing no significant organ damage, mutagenicity, or reproductive toxicity. Low irritation during topical application (cosmetic products); skin irritation tests show no sensitization potential; cytotoxicity tests indicate >98% skin cell survival at concentrations ≤0.1%, suitable for sensitive skin, pregnant women, and other special populations. Compliance meets EU CosIng, China's “List of Cosmetic Ingredients in Use,” and pharmaceutical raw material standards.
United Kingdom