Unclassified
68 compounds in this family, each with its recorded mechanism, routes of administration, safety notes and references to published literature.
- ALY688ALY688 is a synthetic 10‑amino‑acid peptide that mimics adiponectin by activating its cellular receptors. In pre‑clinical studies it has been examined as a tool to improve insulin sensitivity, reduce inflammation and fibrosis, and protect cardiac and skeletal muscle in rodent models of metabolic stress, iron overload, and Duchenne muscular dystrophy. The compound is not approved for any clinical indication and its human safety and efficacy remain untested.
- AmlintideAmlintide is a synthetic version of the pancreatic beta‑cell hormone amylin. It has been investigated in a small human study to characterize its distribution volume, clearance, and residence time after intravenous administration. The compound’s therapeutic role and regulatory status remain undefined.
- Anvatabart opadotin
- AP-102
- AstodrimerAstodrimer (also known as astodrimer sodium, SPL7013, or VivaGel) is a synthetic, polyanionic carbosilane dendrimer formulated as a topical gel for the treatment of bacterial vaginosis (BV) and, more recently, as a nasal spray with antiviral intent. It is a prescription‑only product approved for vaginal use and is being investigated for respiratory virus prevention.
- BPI-3016BPI-3016 is a newly engineered human glucagon‑like peptide‑1 (GLP‑1) analogue designed for the treatment of type 2 diabetes mellitus. Structural modifications give it high resistance to dipeptidyl peptidase‑IV (DPP‑IV) and extend its circulating half‑life, allowing the potential for once‑weekly dosing. Preclinical studies in diabetic mice and cynomolgus monkeys report sustained reductions in fasting and post‑prandial glucose, weight loss, and improved beta‑cell function.
- C326C326 denotes a cysteine residue at position 326 found in several human proteins, including the m6A methyltransferase METTL3, the glycolytic enzyme PKM2, the iron exporter ferroportin, and the E3 ligase FBXO22. Across recent studies, this thiol side chain serves as a reactive hotspot for post‑translational modifications such as S‑nitrosylation, sulfhydration, and covalent binding by small‑molecule degraders, thereby influencing protein stability, enzymatic activity, and cellular signaling pathways.
- Calcium pangamateCalcium pangamate, occasionally referred to as vitamin B15, is a calcium salt of pangamic acid that has been investigated for several pharmacological actions. Early clinical observations suggested it may raise high‑density lipoprotein (HDL) cholesterol in patients with cerebral arteriosclerosis, while animal experiments reported protective effects on liver cells after toxic injury. A small human trial using the related compound dimethylglycine (DMG) reported enhanced antibody responses to vaccination, leading to interest in possible immunomodulatory properties.
- Conestat alfaConestat alfa is a recombinant human C1‑esterase inhibitor (rhC1‑INH) approved for intravenous use in the treatment of acute hereditary angioedema (HAE) attacks. It replaces deficient C1‑INH, thereby restoring regulation of the complement, kallikrein‑kinin, fibrinolytic and coagulation pathways that underlie bradykinin‑mediated swelling. Clinical investigations have also explored its use during prodromal symptoms and as a prophylactic agent to prevent attacks.
- CTB001CTB001 is a recently developed generic version of the anticoagulant bivalirudin. In a phase‑1, single‑dose, dose‑escalation study involving 24 healthy Korean men, its pharmacokinetic (PK) profile and pharmacodynamic (PD) effects on clotting times were characterized using population modelling and simulation. The data provide an initial understanding of how CTB001 behaves in the body and its impact on laboratory measures of coagulation, informing future dosing considerations.
- Demplatin pegraglumer
- EGEN-001EGEN-001 is a plasmid DNA construct encoding interleukin‑12 (IL‑12) that is delivered intraperitoneally using a PEG‑PEI‑cholesterol lipopolymer carrier. In a phase II trial it was tested in women with platinum‑resistant recurrent epithelial ovarian, fallopian tube or primary peritoneal cancer to assess safety and antitumor activity.
- ElamipretideElamipretide (also known as SS‑31, MTP‑131, Bendavia) is an investigational synthetic tetrapeptide that targets mitochondria. It is being studied for conditions linked to mitochondrial dysfunction such as Barth syndrome, heart failure, neurodegeneration, metabolic disorders, and retinal diseases like age‑related macular degeneration. The compound is administered by injection (intravenous or subcutaneous) and remains under clinical investigation, with no regulatory approval for any indication.
- ElobixibatElobixibat is an orally administered prescription drug that inhibits the ileal bile acid transporter (IBAT). By blocking bile‑acid reabsorption, it increases colonic bile‑acid concentrations, which promotes fluid secretion and intestinal motility. It is approved for chronic constipation and is being investigated for constipation associated with Parkinson's disease.
- EmodepsideEmodepside is a cyclic depsipeptide anthelmintic approved for veterinary use in cats and dogs. It has a broad spectrum of activity against gastrointestinal, lung and filarial nematodes and is being repurposed for human infections such as onchocerciasis, trichuriasis and hookworm. Pre‑clinical studies show macrofilaricidal effects, and early human trials suggest dose‑dependent cure rates superior to albendazole.
- EnarodustatEnarodustat is an orally administered hypoxia‑inducible factor prolyl‑hydroxylase (HIF‑PH) inhibitor approved in Japan for treating anemia associated with chronic kidney disease (CKD), both in patients on dialysis and those not on dialysis. By enhancing the body’s own production of erythropoietin and improving iron handling, it aims to raise and maintain hemoglobin levels without the need for injectable erythropoiesis‑stimulating agents.
- EpitalonEpitalon is a synthetic tetrapeptide (Ala‑Glu‑Asp‑Gly) derived from pineal‑gland extracts and studied as a research compound for geroprotective, neuroendocrine, and retinal applications. Researchers investigate its ability to influence aging‑related pathways, boost melatonin production, support immune function, and protect retinal cells.
- FlovagatranFlovagatran is an experimental parenteral anticoagulant that directly inhibits thrombin (factor IIa). It has been investigated as a potential agent for the prevention and treatment of venous thromboembolism, aiming to complement or replace existing injectable anticoagulants such as heparin and low‑molecular‑weight heparin.
- GallichromeGallichrome is a gallium(III) analogue of the microbial siderophore ferrichrome, a cyclic hexapeptide that chelates metal ions. In research, it serves as a stable, diamagnetic surrogate for ferrichrome, allowing detailed structural and biophysical studies of bacterial iron‑uptake proteins such as the periplasmic binding protein FhuD.
- GB-115GB‑115 is a synthetic dipeptide that mimics the tetrapeptide cholecystokinin‑4 (CCK‑4). Pre‑clinical studies in mice and rats have shown it to produce anxiolytic effects after oral or intraperitoneal dosing, to stimulate immune functions such as macrophage phagocytosis, and to enhance morphine‑induced analgesia. All evidence comes from animal experiments; no human trials or regulatory approvals have been reported.
- Glaspimod
- GlyphosateGlyphosate is a non‑selective, systemic herbicide widely used to control weeds in agriculture and landscaping. It acts by inhibiting a plant‑specific enzyme in the shikimate pathway, preventing synthesis of essential aromatic amino acids. While effective for crop protection, concerns have arisen about possible health effects in humans exposed occupationally or through residues in food and water.
- Gonyautoxin IIGonyautoxin II (GTX II) is a naturally occurring paralytic shellfish toxin produced by certain dinoflagellates and accumulated in marine organisms such as crabs. It belongs to the bis‑guanidinium family of toxins that potently block voltage‑gated sodium channels, leading to rapid neurotoxic effects. In research, GTX II is employed as a high‑affinity tool to study sodium channel function and the mechanisms of paralytic shellfish poisoning.
- GS-9256GS-9256 is an oral, phosphinic‑acid‑derived macrocyclic inhibitor of the hepatitis C virus (HCV) NS3/4A serine protease. Developed by Gilead Sciences, it has progressed through preclinical testing and early‑phase clinical studies for chronic genotype‑1 HCV infection, often in combination with other direct‑acting antivirals or pegylated interferon‑ribavirin regimens.
- Icrocaptide
- IMT-288
- ISF402ISF402 (VHTD‑amide) is a synthetic tetrapeptide derived from the urinary peptide GHTD‑amide. In pre‑clinical work it has been investigated as an adjunct to insulin therapy, aiming to improve insulin’s glucose‑lowering effect by altering insulin’s zinc‑dependent aggregation state.
- Isospaglumic acidIsospaglumic acid (N‑acetylaspartylglutamic acid) is mentioned in a 1993 review as a mast‑cell stabiliser considered for topical use in seasonal allergic rhinitis. It is proposed to be part of an individualized treatment strategy that combines allergen avoidance, topical corticosteroids, antihistamines and immunotherapy, aiming to reduce the inflammatory response that underlies nasal allergy symptoms.
- Lagatide
- Maxy-G34Maxy‑G34 is a novel polyethylene glycol‑linked derivative of human granulocyte colony‑stimulating factor (G‑CSF). Developed as a medical countermeasure, it is designed to stimulate neutrophil production and improve survival after acute radiation exposure. Pre‑clinical work has evaluated its pharmacokinetics, pharmacodynamics and efficacy in rodent models of neutropenia and lethal radiation. Studies in mice and rats have shown that a single injection given one day after irradiation can increase survival at doses far lower than conventional G‑CSF, while in chemotherapy‑induced neutropenia models Maxy‑G34 produced a faster and more sustained rise in circulating neutrophils compared with pegfilgrastim.
- Mdl 101,146MDL 101,146 is a synthetic peptidyl electrophilic ketone that acts as a potent, reversible inhibitor of human neutrophil elastase (HNE). Developed in the 1990s, it has been evaluated in a range of rodent models of inflammatory disease, including collagen‑induced arthritis and HNE‑triggered acute lung injury. The compound is not known to have any regulatory approval and its clinical use remains experimental.
- MGB-BP-3MGB‑BP‑3 is an experimental small‑molecule antibiotic belonging to the Strathclyde Minor Groove Binder (S‑MGB) family. It has progressed to Phase IIa clinical testing for treatment of Clostridioides difficile infection (CDI). In vitro it shows potent activity against Gram‑positive organisms, especially C. difficile, but little activity against Gram‑negative bacteria. Its novelty lies in binding to the minor groove of bacterial DNA and interfering with type II topoisomerases, offering a mechanistically distinct option to existing CDI therapies.
- Mibenratide
- MM3122MM3122 is a small‑molecule ketobenzothiazole inhibitor that targets host serine proteases such as TMPRSS2, matriptase and hepsin. By blocking these enzymes, it prevents activation of the coronavirus spike protein, thereby inhibiting entry of SARS‑CoV‑2, its EG.5.1 subvariant, MERS‑CoV and related viruses into human lung cells. Pre‑clinical studies show potent antiviral activity in cell culture and protective effects in a mouse model of COVID‑19.
- N-[(6S)-6-Carboxy-6-(glycylamino)hexanoyl]-D-alanyl-D-alanine
- NAD+NAD+ (nicotinamide adenine dinucleotide) is an essential coenzyme and signaling molecule central to cellular energy metabolism, redox homeostasis, and enzyme regulation. Not a peptide in strict biochemical definition, but functionally peptide-associated in metabolic and longevity research contexts.
- NagrestipenNagrestipen is an experimental small‑molecule compound identified in a recent transcriptomic analysis of ischemic stroke as a candidate regulator of the chemokine gene Ccl3. The study suggests that, by influencing Ccl3 expression in basophils and their interaction with neutrophils, nagrestipen might affect the senescence‑associated secretory phenotype (SASP) and downstream immune processes that contribute to stroke pathology in humans and animal models.
- NavepegritideNavepegritide (brand name YUVIWEL®) is a long‑acting prodrug of C‑type natriuretic peptide (CNP) approved in the United States for increasing linear growth in children aged two years and older with achondroplasia whose growth plates are still open. It is given once weekly by subcutaneous injection and is being studied for related conditions such as hypochondroplasia.
- Nitrilotriacetic acidNitrilotriacetic acid (NTA) is a small tetradentate chelating agent that forms stable complexes with transition‑metal ions such as Ni²⁺ or Co²⁺. The resulting NTA‑metal complex binds with high (sub‑nanomolar) affinity to poly‑histidine (His‑tag) sequences on recombinant proteins. This reversible interaction underpins a range of research applications, including affinity purification, protein immobilisation, biosensor construction, and the recruitment of His‑tagged proteins to NTA‑functionalised lipids in in‑vitro autophagy assays.
- NN344NN344 (LysB29(Nε‑lithocholyl‑γ‑Glu) des‑B30 human insulin) is a long‑acting basal insulin analogue that incorporates a lithocholic‑acid moiety. The modification promotes self‑assembly into high‑molecular‑weight hexameric rods after subcutaneous injection, creating a depot that releases insulin slowly over more than 24 hours. It has been investigated in animal models and a small randomized human clamp study as a potential once‑daily basal insulin.
- NRP-2945
- P21
- Paclitaxel poliglumexPaclitaxel poliglumex (PPX, also known as XYOTAX or CT‑2103) is an investigational polymer‑drug conjugate that links the chemotherapeutic agent paclitaxel to poly‑L‑glutamic acid. Administered intravenously, the macromolecule is designed to exploit the enhanced permeability and retention effect of tumor vasculature, delivering higher concentrations of active drug to cancer cells while limiting systemic exposure. It has been studied in non‑small cell lung cancer, ovarian cancer and other solid tumours, with early‑phase trials suggesting comparable efficacy to standard paclitaxel but with a different toxicity profile.
- PareptidePareptide is a synthetic analogue of the neuropeptide melanotropin‑inhibiting factor (MIF‑1). It is employed primarily as a research tool to study peptide metabolism, dopaminergic receptor interactions, and the development of tolerance to antipsychotic‑induced catalepsy in rodents. The compound has been characterized in biochemical assays for its stability in brain tissue and quantified in biological fluids using high‑performance liquid chromatography. Its short peptide sequence lacks a C‑terminal amidation, yet retains activity comparable to MIF‑1 in experimental models.
- Pegdinetanib
- PegmusirudinPegmusirudin is an experimental parenteral anticoagulant that belongs to the class of direct thrombin (factor IIa) inhibitors. It is mentioned in a 2011 review of new anticoagulants as a compound under development, intended for prevention or treatment of thromboembolic conditions. No regulatory status or clinical approval is reported in the cited literature.
- PhosphoramidonPhosphoramidon is a research‑grade pseudo‑peptide metalloprotease inhibitor, classified among phosphoramidon‑type compounds. It blocks several zinc‑dependent endopeptidases, notably neprilysin‑like enzymes, endothelin‑converting enzyme (ECE) and endopeptidase‑24.11. In laboratory studies it is used to probe the roles of these enzymes in amyloid‑beta clearance, endothelin production, and opioid peptide metabolism, and to model disease mechanisms in Alzheimer’s disease, Chagas‑related cardiomyopathy, and neuropeptide signaling.
- Pirnabine
- PR-15PR-15 is an experimental platelet glycoprotein VI (GPVI) adhesion antagonist being investigated as a novel antiplatelet agent. It is mentioned in a review of emerging antiplatelet drugs alongside agents such as prasugrel and ticagrelor. No clinical trial data are provided, and its regulatory status, approved indications, or commercial availability are not established.
- Revakinagene taroretcelRevakinagene taroretcel (Encelto™, NT‑501) is an encapsulated cell‑based gene therapy that delivers recombinant human ciliary neurotrophic factor (CNTF) directly into the eye. It is approved in the United States for the treatment of adults with idiopathic macular telangiectasia type 2 and is being investigated for other chronic retinal degenerations.
- RWJ-800088RWJ-800088 is a synthetic, polyethylene‑glycol‑conjugated peptide that mimics thrombopoietin (TPO). It has been investigated as a vascular radioprotectant and as a means to raise platelet counts in thrombocytopenia. Early human studies used a single intravenous dose in healthy volunteers, while pre‑clinical work examined its ability to limit radiation‑induced vascular leakage and inflammation in rodents.
- SaxagliptinSaxagliptin is an oral prescription drug approved for the management of type 2 diabetes mellitus. It belongs to the dipeptidyl peptidase‑4 (DPP‑4) inhibitor class and is sold under brand names such as Onglyza and Kombiglyze XR. By enhancing the body’s own incretin response, saxagliptin helps lower blood glucose levels and is generally weight‑neutral.
- Semparatide
- SER-100SER-100, also known as ZP120, is a synthetic peptide ligand that selectively targets the nociceptin/orphanin FQ (NOP) receptor. It is being explored as a therapeutic candidate for the clinical management of systolic hypertension, based on the role of the NOP system in cardiovascular regulation.
- Skf 107457SKF 107457 is a synthetic hexapeptide analogue designed to inhibit the HIV‑1 protease enzyme. In the described study it was examined as a hydroxyethylene‑based inhibitor, where the scissile peptide bond is replaced by a non‑cleavable hydroxyethylene isostere. The compound was investigated primarily through X‑ray crystallography to understand how it binds the protease, rather than through clinical or pharmacological testing.
- ST-003
- TifuvirtideTifuvirtide (also called T‑1249) is an experimental peptide designed to inhibit HIV‑1 entry by blocking the fusion step between the viral envelope and the host cell membrane. It belongs to the class of HIV‑1 fusion inhibitors and is being investigated as a potential addition to antiretroviral regimens, especially for viruses resistant to existing drugs. Early‑stage studies have placed it in clinical‑trial pipelines alongside other entry blockers.
- Tigapotide
- Timbetasin
- Tiplimotide
- TP-3654TP-3654 is an experimental small‑molecule inhibitor of the PIM family of serine‑threonine kinases, primarily PIM1. Pre‑clinical studies have examined its ability to reduce fibrosis, overcome drug resistance, and enhance the activity of other anticancer agents in models of skeletal‑muscle atrophy, myelofibrosis, acute myeloid leukemia, and renal cell carcinoma. A separate peptide bearing the same identifier has been radiolabelled with Tc‑99m for imaging VIP‑receptor‑positive tumours.
- Tralesinidase alfaTralesinidase alfa is an investigational enzyme replacement therapy designed for mucopolysaccharidosis type IIIB (Sanfilippo syndrome B), a rare pediatric lysosomal storage disorder. The drug is a recombinant fusion of human N‑acetyl‑α‑glucosaminidase (NAGLU) and a modified insulin‑like growth factor‑2 (IGF2) tag, intended to restore the missing lysosomal enzyme activity and reduce heparan‑sulfate buildup in the brain and other tissues.
- TriletideTriletide is a synthetic tripeptide investigated in the mid‑1980s as a cytoprotective agent for peptic ulcer disease. Small randomised trials evaluated oral doses of 1–2 g per day in patients with gastric or duodenal ulcers, reporting accelerated ulcer healing and relief of heartburn, epigastric pain and antacid use. The compound was compared with antacids, ranitidine, cimetidine and carbenoxolone, and was generally well tolerated.
- Vasomera
- Viquidacin
- Viral Macrophage-Inflammatory ProteinViral macrophage‑inflammatory protein‑II (vMIP‑II) is a small chemokine encoded by human herpesvirus‑8. It acts as a broad‑spectrum modulator of chemokine receptors, capable of both antagonising many inflammatory pathways and agonising select receptors such as CCR8. Pre‑clinical studies have used vMIP‑II to dampen leukocyte recruitment in organ transplantation, reduce brain infarct size after stroke, and enhance the therapeutic targeting of engineered extracellular vesicles for viral myocarditis.
- VM4-037VM4-037 is a small‑molecule radiotracer labelled with fluorine‑18 (^18F‑VM4-037) designed for positron emission tomography (PET) imaging of carbonic anhydrase IX (CA‑IX), a protein over‑expressed in hypoxic tumours and clear‑cell renal cell carcinoma (ccRCC). The compound is investigated as a non‑invasive marker of CA‑IX expression and tumour hypoxia, primarily for detecting metastatic disease and for research into CA‑IX‑targeted theranostics.
- Xempritolimod