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.

Dabigatran etexilate (BIBR 1048) is a thrombin inhibitor that binds to thrombin, blocking its thrombogenic activity and preventing thrombus formation.

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

Clindamycin Phosphate is the phosphate salt form of clindamycin, a semi-synthetic, chlorinated broad-spectrum antibiotic produced by chemical modification of lincomycin. Clindamycin phosphate (Clindamycin 2-dihydrogen phosphate) is used in topical preparations.

Mestranol (Devocin), a semisynthetic estrogen, is used as an estrogen receptor agonist and must be demethylated to be biologically active.

Adefovir dipivoxil (GS 0840) is a dipivoxil formulation of adefovir, a nucleoside reverse transcriptase inhibitor analog of adenosine with activity against hepatitis B virus (HBV), herpes virus, and human immunodeficiency virus (HIV).

Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug being developed for delivering nicotinic acid (NIC) into the skin to prevent actinic keratosis and its progression to skin cancer.

Isavuconazole (RO-0094815)(BAL-4815; RO-0094815) is the active component of the new azole antifungal agent BAL8557 with MIC(50)s/MIC(90)s ranged from 0.002/0.004 mg/liter for C. albicans to 0.25/0.5 mg/liter for C. glabrata.

Dabigatran Etexilate Mesylate (BIBR 1048MS) is the orally active prodrug of dabigatran. Dabigatran is a reversible and selective, direct thrombin inhibitor (DTI, Ki: 4.5 nM).

Methyldopa hydrate (MK-351 hydrate) is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension. It inhibits the sympathetic nervous system, decreases production of dopamine, norepinephrine, and epinephrine, and exhibits NO-dependent sedative activity.

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

Dipivefrin hydrochloride (Dipivefrin HCl) that is available as an ophthalmic solution is a prodrug of adrenaline, which is used to treat glaucoma.

Valecobulin hydrochloride (CKD-516 hydrochloride) is the valine prodrug and vasoblocker of S516. Valecobulin hydrochloride (CKD-516 hydrochloride) has a potent inhibitory effect on β-tubulin polymerization and has significant anti-tumor activity against solid tumors in mice and humans.

Dexamethasone palmitate (DXP), a lipophilic prodrug of Dexamethasone, shows a 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone. Dexamethasone palmitate is a glucocorticoid receptor agonist and an anti-inflammatory agent.

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 hydrochloride (L-DOPA ethyl ester) is a prodrug of levodopa. It also has greater gastric solubility and significant brain penetration.

Isavuconazonium sulfate is hydrolyzed by plasma esterases to yield the active moiety isavuconazole. Isavuconazole binds to and inhibits the fungal cytochrome P450 family enzyme lanosterol 14-alpha-demethylase (CYP51), which catalyzes the demethylation of

Ceftobiprole medocaril (BAL5788), the parenteral prodrug of Ceftobiprole, is a broad-spectrum cephalosporin effective against Methicillin-resistant Staphylococcus aureus (MRSA).

Ceftaroline fosamil (TAK-599) is a cephalosporin, with activity against Gram-positive pathogens.

2',3',5'-triacetyl-5-Azacytidine (Nsc291930) is a prodrug form of 5-azacytidine that may be rapidly absorbed orally.

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.

Brincidofovir (HDP-CDV) is an orally active, lipophilic form of cidofovir. It has enhanced activity compared to CDV against certain adenoviruses, herpesviruses, and orthopoxviruses.

Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a microtubule polymerization inhibitor prodrug mediated by Pd. Developed from colchicine-binding site inhibitors (CBSIs), it aims to reduce toxicity and enhance targeted release. Compared to the parent compound, its cytotoxicity is decreased by 68.3 times, but can be in situ restored in the presence of Pd resin. Mechanistic studies show it retains the same antitumor activity as CBSIs. In vivo tests demonstrate that, once activated by Pd resin, it significantly suppresses tumor growth (63.2% inhibition rate). Tubulin Polymerization-IN-1 prodrug is a promising candidate for cancer research.

TrxR1 prodrug-1 (compound 5u) is a potent inhibitor of TrxR1, demonstrating significant antitumor activity in nude mice and NSCLC organoids.