prodrug

Etoposide (VP-16-213) is a topoisomerase II inhibitor that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA (IC50=60.3 μM). Etoposide has antitumor activity and induces apoptosis and autophagy.

Testosterone acetate (NSC-523836) is a hormone with in vitro antitumor activity.

Methyldopa (MK-351), an alpha-adrenergic agonist (selective for α2-adrenergic receptors) psychoactive medicine, is served as an antihypertensive or sympatholytic.

L-DOPA (Levodopa) is an amino acid precursor of dopamine with antiparkinsonian properties. It is a prodrug converted to dopamine by DOPA decarboxylase and can cross the blood-brain barrier. In the brain, levodopa is decarboxylated to dopamine, stimulating dopaminergic receptors and compensating for depleted endogenous dopamine in Parkinson's disease. To ensure adequate concentrations reach the central nervous system, levodopa is administered with carbidopa, a decarboxylase inhibitor that does not cross the blood-brain barrier, reducing peripheral decarboxylation and increasing CNS dopamine delivery.

Irinotecan Hydrochloride (CPT-11 hydrochloride) is the hydrochloride salt of a semisynthetic derivative of camptothecin. Irinotecan, a prodrug, is converted to a biologically active metabolite 7-ethyl-10-hydroxy-camptothecin (SN-38) by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, SN-38 inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Because ongoing DNA synthesis is necessary for irinotecan to exert its cytotoxic effects, it is classified as an S-phase-specific agent.

Succinic anhydride is a cyclic anhydride. Succinic anhydride acts as a nonclaevable ADC linker. Succinic anhydride can react with compound 4 to link the prodrug to an amine or hydroxy 1 group of a targeting polypeptide.

Fosbretabulin Disodium (CA 4P), a water-soluble prodrug of Combretastatin A4 (CA4), is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). Fosbretabulin Disodium(Combretastatin A4 disodium phosphate) inhibits the polymerization of tubulin (IC50: 2.4 μM), and also disrupts tumor vasculature.

3-Sulfopropanoic acid, a major metabolite of treprostinil and its prodrug ALZ-801, is an endogenous molecule present in the cerebrospinal fluid (CSF) of AD patients that inhibits the formation of Aβ42 oligomers.

MRE-269 (ACT-333679) is an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269(ACT-333679) is used for the treatment of pulmonary arterial hypertension. MRE-269(ACT-333679) is an active metabolite of Selexipag (S253150).

Diacerein (Fisiodar) is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including sevre diarrhea [L780]. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.

EGCG Octaacetate, a prodrug of EGCG, is utilized to enhance the stability and bioavailability of EGCG in vivo. It has high efficacy, bioavailability, anti-oxidation, and anti-angiogenesis capacities.

Chloramphenicol succinate is a water-soluble prodrug of Chloramphenicol, a bacteriostatic antibiotic that binds to bacterial ribosomes to block their translation. CPSA is a competitive substrate and inhibitor of succinate dehydrogenase (SDH). In vitro, Kemicetine succinate can be oxidized by succinate dehydrogenase to release chloramphenicol.

Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. It diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into cells in vivo, exhibiting potent proapoptotic, antiproliferative, and differentiation-inducing effects.

Etilevodopa is an ethyl-ester prodrug of Levodopa which is used for the treatment of Parkinson's disease (PD). It is rapidly hydrolyzed to Levodopa and ethanol by nonspecific esterases in the gastrointestinal tract. Levodopa is the direct precursor of dop