Aptiganel
Molecular Formula: C₁₄₇H₂₃₈N₄₄O₄₂S
Molecular Weight: 3326.08
Amino Acid Sequence: His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Leu-Asn-NH₂
Appearance: White powder
Actions:
Vascular Regulation: It can cause vasodilation and lower blood pressure. It has a relatively strong effect on visceral blood vessels but no effect on the femoral artery.
Digestive Function Regulation: It can promote the secretion of intestinal juice, has a relatively weak promoting effect on pancreatic secretion, can inhibit the secretion of gastric juice, and can also inhibit the contraction of the smooth muscles in the digestive tract.
Other Actions: It is one of the signaling molecules in the neuroendocrine immune network and has the characteristics of anti-proliferation, anti-inflammation, and immunomodulation. In various animal models of respiratory distress, acute lung injury, and inflammation, it shows powerful anti-cytokine activity.
Clinical Application Prospects
Respiratory System Diseases: Four of its indications have been granted the title of FDA orphan drug designation, namely acute respiratory distress syndrome, pulmonary hypertension, acute lung injury, and sarcoidosis. However, in the treatment of severe COVID-19, Aptiganel was twice rejected by the FDA for emergency use authorization (EUA) in 2022, and it also failed in a Phase III clinical trial for severe COVID-19 patients.
Digestive System Diseases: It can be used to treat some diseases related to abnormal secretion of digestive juices and gastrointestinal motility, such as functional dyspepsia, irritable bowel syndrome, etc. It regulates the secretion of digestive juices and gastrointestinal peristalsis to improve relevant symptoms.
Storage Conditions: Generally, it needs to be lyophilized and stored in the dark at - 20°C.