Fozivudine tidoxil is a thioether lipid–Zidovudine (ZDV) conjugate. After intake it is split intracellularly into the lipid moiety and ZDV-monophosphate, which is subsequently phosphorylated to the active metabolite ZDV-triphosphate. The rationale behind the development of fozivudine (FZD) was to take advantage of the high cleavage activity in mononuclear cells and other organs resulting in increased amounts of intracellular ZDV available for phosphorylation to the active metabolite, and a very low activity in red blood and stem cells, which should result in reduced haematologic toxicity. It is member of the family of nucleoside reverse transcriptase (RT) inhibitors. Fozivudine tidoxil has been in Phase II clinical trials for the treatment of HIV infection. There were three adverse events possibly related to fozivudine: urine abnormality, gastrointestinal pain and abnormal dreams.

Mannose 6-phosphate (M6P) has type-I integral membrane receptors. M6P-receptors bind and transport M6P-enzymes to lysosomes, but it can also modulate the activity of a variety of extracellular M6P-glycoproteins (i.e., latent TGFbeta precursor, urokinase-type plasminogen activator receptor, Granzyme B, growth factors, Herpes virus). M6P has been demonstrated to reduce active TGF-β1 expression on cultured tendon fibroblasts and improved range of movement in a rabbit flexor tendon injury model. Studies of M6P in relation to skin scarring demonstrate improvement in scar cosmesis and accelerated return of normal dermal architecture. Juvidex, a formulation of M6P, inhibits the activation of TGF-beta1 and TGF-beta2, which are present at high levels in adult wounds that scar. On the other hands, M6P in a 600 mM hypertonic solution (Adaprev) potentially acts via a physical, non-chemical, hyperosmotic effect.

1-(3,5-BIS-O-(BUTOXYHYDROXYPHOSPHINYL)-2-DEOXY-D-ERYTHRO-PENTOFURANOSYL)-5-METHYL-2,4(1H,3H)-PYRIMIDINEDIONE (Nu-3), a Bisphosphocins, is being developed by Lakewood-Amedex (formerly Nu Pharmas), for the treatment of diabetic foot ulcer, lung infections, stomatitis. Nu-3, a novel synthetic broad-spectrum antimicrobial proven to be effective in killing a wide range of Gram-positive, Gram-negative and antibiotic-resistant bacteria, recently completed a Phase 1/2a clinical trial in patients, showing no treatment-related adverse events and a trend toward efficacy. Patients treated with 2% Nu-3 for seven days had a 65.5% reduction in ulcer area versus a 29.9% reduction in the placebo arm, as measured 14 days after treatment began. In addition, 62.5% of patients treated with 2% Nu-3 saw a reduction in the microbiological load, versus 20% in the placebo. Three additional Phase 2a adaptive arm clinical trials providing robust clinical data in areas of urgent medical need are expected to be completed by 2020.

Oxi0-4503 (now known as combretastatin A1 phosphate), a diphosphate prodrug of combretastatin A1, was developed by Mateon therapeutics as a second-generation, dual-mechanism vascular disrupting agent from the combretastatin family. On November 21, 2012, Oxi-4503 has been granted orphan designation by the US Food and Drug Administration for the treatment of acute myelogenous leukemia. It is known that the orphan drug designation qualifies a company for several benefits, including the potential for market exclusivity, development grants, and tax credits. Oxi0-4503 is currently participating in phase I/II clinical trial the treatment of patients with acute myelogenous leukemia or myelodysplastic syndrome. In addition, phase I clinical trial was successfully completed where was studied the safety of Oxi0-4503 in patients with advanced solid tumors.

Defoslimod is an analog of lipopolysaccharide endotoxin-derived lipid A obtained from E. coli, developed as an immunomodulatory adjuvant and an immunotherapeutic agent for the treatment of cancer. Defoslimod acts as an agonist of Toll-like receptor (TLR) 2/4. In a phase 1 clinical study in patients with solid tumors, conducted in 2007, defoslimod was administered as an intravenous infusion. The therapy was well tolerated at biologically active concentrations, with 3 patients of 17 exhibited disease stabilization with a mean duration of 4 months. No further development of the drug was reported.

1,​2-​Dioleoyl-​sn-​glycero-​3-​phospho-​L-​serine Sodium Salt is a lipid being studied in the assembly and long-term stability of solid supported lipid bilayers from artificial and natural lipid mixtures.