Evidence Grade B — Strong clinical evidence. 322 published studies, 115 human. 2 registered clinical trials.
Medically reviewed by a licensed medical professional
Dalargin is a synthetic opioid peptide developed in the Soviet Union in the 1980s for peptic ulcer exacerbations and acute pancreatitis. The clinical evidence base is predominantly from Russian-language publications and has not undergone Western regulatory review.
Dalargin is also known by these brand and alternate names:
322 published studies: 115 human, 194 animal, 29 in-vitro, 9 reviews
Dalargin is approved in Russia for peptic ulcer exacerbations, acute pancreatitis, and pancreatic necrosis. It has not been approved by the FDA, EMA, or other major Western regulatory agencies.
The clinical evidence base is predominantly from Russian publications. The development history spans the 1980s Soviet pharmaceutical research programme. The clinical evidence has not undergone Western regulatory review. Its regulatory status is limited to Russia and certain former Soviet states.
Research suggests dalargin acts on opioid receptors, though its receptor selectivity profile has been debated — initially classified as a delta-opioid agonist, later research suggested preferential mu-opioid activity. Proposed gastroprotective effects include stimulation of mucosal repair processes. These mechanisms are based on pharmacological studies, primarily from Russian institutions.
Research suggests the evidence base for dalargin consists primarily of Russian and Soviet-era literature from the 1980s and 1990s, mostly in Russian-language journals. No internationally standardised clinical trials, no head-to-head comparisons with modern treatments (such as proton pump inhibitors), and no Western regulatory review exist. Over 35 years of clinical use in Russia provides pragmatic evidence of some utility, but this does not constitute rigorous proof by modern international standards. The compound's receptor selectivity remains disputed between different research groups. For these reasons, it is classified as a research compound.
PeptideTrace tracks 2 registered clinical trials for Dalargin sourced from ClinicalTrials.gov.
Dalargin for Prevention of Organ Disfunction in High-Risk Abdominal Surgery
An Open Randomized Study of Dalargin Efectiveness in Combination With Leitragin Drug in Patients With Severe and Critical Manifestations of SARS-COVID-19
Dalargin is a synthetic hexapeptide leu-enkephalin analogue developed in the 1980s at the laboratory of peptide synthesis of the All-Russian Scientific Center (VKNC) of the USSR Academy of Medical Sciences under Prof. M.I. Titov. Sequence: Tyr-D-Ala-Gly-Phe-Leu-Arg. Molecular weight: 725.85 Da. CAS: 81733-79-1. Molecular formula: C35H51N9O8. The D-Ala2 substitution confers enzymatic stability, while the C-terminal arginine restricts blood-brain barrier penetration, confining activity to the periphery. Russian pharmaceutical registration: P N001319/01-231209. Formulated as 1 mg lyophilizate ampoules for IV/IM injection. Approved in Russia for peptic ulcer exacerbations (duodenal and stomach), acute pancreatitis, and pancreatic necrosis. Not approved by any Western regulatory agency.
Research suggests dalargin's receptor selectivity is more complex than initially described. Originally classified as a delta-opioid receptor agonist, the landmark Pencheva et al. study (Br J Pharmacol 1999; PMC1571668) found it showed preferential mu-opioid activity over delta-activity in guinea-pig myenteric plexus assays. The cytoprotective mechanism involves suppression of proteolysis, moderate antisecretory activity, and suppression of pancreatic exocrine secretion. Research suggests the C-terminal arginine is essential for cytoprotective activity. The NO system plays a role: the NO synthase inhibitor L-NAME abolished dalargin's effects on DNA synthesis in gastric mucosal epithelium. Research suggests dalargin does not cross the BBB, which made it a model compound for nanoparticle-mediated drug delivery research (Kreuter et al.): PBCA nanoparticles coated with polysorbate 80 enabled central analgesic effects.
Dalargin is an approved pharmaceutical in Russia for peptic ulcer exacerbations, acute pancreatitis, and pancreatic necrosis. Key development publications include Titov et al. (1985; PMID 2998416), Smagin et al. (1987; PMID 3554590), and Vinogradov and Polonskii (1988; PMID 3067406), summarizing 5 years of clinical development. Preclinical studies demonstrate stimulation of DNA synthesis in gastric mucosa (Lebedko et al., 2007) and protection against NSAID gastropathy (Zhivotova et al., 2009). The optimal preclinical dose was 10 ug/kg, with a bell-shaped dose-response curve. In nanoparticle drug delivery research, Kreuter et al. demonstrated that PBCA nanoparticles with polysorbate 80 coating enabled dalargin to cross the BBB and produce central analgesic effects, establishing a foundational paradigm in nanoparticle drug delivery.
The information on this page is provided for educational and research reference purposes only. This is not medical advice. Always consult a qualified healthcare professional before making any health-related decisions.
Linaclotide is marketed as Linzess (approved August 2012). It is taken as a daily oral capsule on an empty stomach, at least 30 minutes before the first meal. The recommended dose is 290 mcg for IBS-C and 72 or 145 mcg for chronic constipation. In clinical trials, approximately 34% of IBS-C patients met the composite improvement endpoint compared to 17% on placebo. Diarrhoea is the most common side effect (approximately 20%) and the leading reason for discontinuation. Linaclotide has a boxed warning against use in children under 6 years due to deaths in young mice, though no such events have been reported in humans. It competes with plecanatide (which targets the same pathway) and other IBS-C treatments.
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This content is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before making decisions about your health.
