Drug results: 45
| sulindac | A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects. |
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| foscarbidopa | Foscarbidopa and foslevodopa combination (ABBV-951) was aproved by PMDA for the treatment of motor fluctuations in patients with advanced Parkinson’s disease. Foscarbidopa and foslevodopa are prodrugs of carbidopa and levodopa, respectively. They have higher solubility than their parent compounds, which allows them to be administered as a continuous subcutaneous infusion. |
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| ampiroxicam | prodrug of piroxicam; structure given in first source |
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| docarpamine | a dopamine prodrug; RN given refers to (S)-isomer; structure given in first source |
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| tedizolid phosphate | Tedizolid phosphate is a prodrug that is converted by phosphatases to tedizolid, the microbiologically active moiety, following oral and intravenous administration. The antibacterial activity of tedizolid is mediated by binding to the 50S subunit of the bacterial ribosome resulting in inhibition of protein synthesis. Tedizolid inhibits bacterial protein synthesis through a mechanism of action different from that of other non-oxazolidinone class antibacterial drugs; therefore, cross-resistance between tedizolid and other classes of antibacterial drugs is unlikely. |
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| tenofovir alafenamide | a phosphonoamidate prodrug of tenofovir (2'deoxyadenosine monophosphate analog). Plasma exposure to tenofovir alafenamide allows for permeation into cells and then tenofovir alafenamide is intracellularly converted to tenofovir through hydrolysis by cathepsin A. Tenofovir is subsequently phosphorylated by cellular kinases to the active metabolite tenofovir diphosphate. Tenofovir diphosphate inhibits HIV replication through incorporation into viral DNA by the HIV reverse transcriptase, which results in DNA chain-termination |
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| capecitabine | A deoxycytidine derivative and fluorouracil PRODRUG that is used as an ANTINEOPLASTIC ANTIMETABOLITE in the treatment of COLON CANCER; BREAST CANCER and GASTRIC CANCER. |
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| etoposide phosphate | Etoposide phosphate is a prodrug that is converted to its active moiety, etoposide, by dephosphorylation. Etoposide causes the induction of DNA strand breaks by an interaction with DNA-topoisomerase II or the formation of free radicals, leading to cell cycle arrest, primarily at the G2 stage of the cell cycle, and cell death. |
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| cilazapril | One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors) used for hypertension. It is a prodrug that is hydrolyzed after absorption to its main metabolite cilazaprilat. |
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| deflazacort | Deflazacort is a corticosteroid prodrug, whose active metabolite, 21-desDFZ, acts through the glucocorticoid receptor to exert anti-inflammatory and immunosuppressive effects. The precise mechanism by which deflazacort exerts its therapeutic effects in patients with Duchenne muscular dystrophy is unknown. |
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| parecoxib | Parecoxib is a prodrug of valdecoxib. Valdecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor within the clinical dose range. Cyclooxygenase is responsible for generation of prostaglandins. Two isoforms, COX-1 and COX-2, have been identified. COX-2 is the isoform of the enzyme that has been shown to be induced by pro-inflammatory stimuli and has been postulated to be primarily responsible for the synthesis of prostanoid mediators of pain, inflammation, and fever. |
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| ceftobiprole medocaril | a ceftobiprole prodrug |
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| chloramphenicol succinate | inactive precursor (PRODRUGS) of chloramphenicol; used for parenteral administration of chloramphenicol; RN given refers to (R-(R*,R*))-isomer |
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| terlipressin | Terlipressin is a synthetic vasopressin analogue with twice the selectivity for vasopressin V1 receptors versus V2 receptors. Terlipressin acts as both a prodrug for lysine-vasopressin, as well as having pharmacologic activity on its own. Terlipressin is thought to increase renal blood flow in patients with hepatorenal syndrome by reducing portal hypertension and blood circulation in portal vessels and increasing effective arterial volume and mean arterial pressure (MAP). It is used to control bleeding of ESOPHAGEAL VARICES and for the treatment of HEPATORENAL SYNDROME. |
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| valganciclovir | Valganciclovir is an L-valyl ester (prodrug) of ganciclovir that exists as a mixture of two diastereomers. After oral administration, both diastereomers are rapidly converted to ganciclovir by intestinal and hepatic esterases. Ganciclovir is a synthetic analogue of 2'-deoxyguanosine, which inhibits replication of human CMV in cell culture and in vivo. |
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| balsalazide | a mesalamine 5-aminosalicylate prodrug; 99% of ingested drug remains intact through the stomach and is delivered to and activated in the colon; used for inflammatory bowel disease, ulcerative colitis and radiation-induced proctosigmoiditis but avoided in patients with known hypersensitivity reaction to salicylates or mesalamine |
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| secnidazole | Secnidazole is a 5-nitroimidazole antimicrobial. 5-nitroimidazoles enter the bacterial cell as an inactive prodrug where the nitro group is reduced by bacterial enzymes to radical anions. It is believed that these radical anions interfere with bacterial DNA synthesis of susceptible isolates. |
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| aripiprazole lauroxil | prodrug of aripiprazole, following intramuscular injection is converted by enzyme-mediated hydrolysis to N-hydroxymethyl aripiprazole which is then hydrolyzed to aripiprazole |
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| amprenavir | ; RN refers to (3S-(3R*(1S*,2R*)))-isomer; fosamprenavir is a prodrug |
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| gabapentin enacarbil | Gabapentin enacarbil is a prodrug of gabapentin and, accordingly, its therapeutic effects in restless legs syndrome and postherpetic neuralgia are attributable to gabapentin. In animal models of analgesia, gabapentin prevents allodynia (pain-related behavior in response to a normally innocuous stimulus) and hyperalgesia (exaggerated response to painful stimuli). |
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| omidenepag isopropyl | Omidenepag isopropyl is a prodrug that is converted by hydrolysis to omidenepag, the active form that it is thought to lower ophthalmic pressure via a dual mechanism of action, increasing both the trabecular outfow facility and the uveoscleral outfow as a result of EP2 receptor stimulation, thereby promoting aqueous outfow. |
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| faropenem medoxil | a faropenem prodrug for treating bacterial infections |
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| serdexmethylphenidate | Serdexmethylphenidate is a prodrug of dexmethylphenidate (d-MPH). The mode of therapeutic action in ADHD is not known. Serdexmethylphenidate is not deemed to have pharmacological activity until converted to d-MPH. Dexmethylphenidate HCl is a central nervous system (CNS) stimulant that blocks the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. |
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| fosinopril | A phosphinic acid-containing angiotensin-converting enzyme inhibitor that is effective in the treatment of hypertension. It is a prodrug that is converted to its active metabolite fosinoprilat. |
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| propacetamol | prodrug for acetaminophen |
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| erythromycin acistrate | prodrug of erythromycin; 2'-acetyl ester & stearate salt of erythromycin |
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| foslevodopa | Foslevodopa and foscarbidopa combination (ABBV-951) was aproved by PMDA for the treatment of motor fluctuations in patients with advanced Parkinson’s disease. Foscarbidopa and foslevodopa are prodrugs of carbidopa and levodopa, respectively. They have higher solubility than their parent compounds, which allows them to be administered as a continuous subcutaneous infusion. |
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| fosfluconazole | prodrug of fluconazole |
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| nelarabine | prodrug of ara-G |
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| bacampicillin | ester prodrug that is hydrolyzed to ampicillin after its absorption from the gastrointestinal tract; RN given refers to parent cpd; structure |
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| alatrofloxacin | prodrug of trovafloxacin |
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| mycophenolate mofetil | Mycophenolate mofetil is a prodrug of mycophenolic acid, an inhibitor of inosine-5'-monophosphate dehydrogenase. MPA depletes guanosine nucleotides preferentially in T and B lymphocytes and inhibits their proliferation. |
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| valaciclovir | A prodrug of acyclovir that is used in the treatment of HERPES ZOSTER and HERPES SIMPLEX VIRUS INFECTION of the skin and mucous membranes, including GENITAL HERPES. |
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| fostemsavir | Fostemsavir is a prodrug without significant biochemical or antiviral activity that is hydrolyzed to the active moiety, temsavir, which is an HIV-1 attachment inhibitor. Temsavir binds directly to the gp120 subunit within the HIV-1 envelope glycoprotein gp160 and selectively inhibits the interaction between the virus and cellular CD4 receptors, thereby preventing attachment. Additionally, temsavir can inhibit gp120-dependent post-attachment steps required for viral entry into host cells. |
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| tenofovir disoproxil | Tenofovir disoproxil fumarate is the fumarate salt of the prodrug tenofovir disoproxil. Tenofovir disoproxil is absorbed and converted to the active substance tenofovir, which is a nucleoside monophosphate (nucleotide) analogue. Tenofovir is then converted to the active metabolite, tenofovir diphosphate, an obligate chain terminator, by constitutively expressed cellular enzymes. Tenofovir diphosphate has an intracellular half-life of 10 hours in activated and 50 hours in resting peripheral blood mononuclear cells (PBMCs). Tenofovir diphosphate inhibits HIV-1 reverse transcriptase and the HBV polymerase by direct binding competition with the natural deoxyribonucleotide substrate and, after incorporation into DNA, by DNA chain termination. Tenofovir diphosphate is a weak inhibitor of cellular polymerases alpha, beta, and gamma. At concentrations of up to 300 umol/l, tenofovir has also shown no effect on the synthesis of mitochondrial DNA or the production of lactic acid in in vitro assays. |
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| cefpodoxime proxetil | Prodrug for cefpodoxime |
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| benazepril | prodrug of benazeprilat inhibit angiotensin-converting enzyme (ACE) and results in decreased plasma angiotensin II, which leads to decreased vasopressor activity and to decreased aldosterone secretion |
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| famciclovir | An aminopurine derivative and prodrug of penciclovir which is a competitive inhibitor of herpes simplex 2 DNA polymerase. It is used to treat HERPES SIMPLEX VIRUS INFECTION. |
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| fosamprenavir | a prodrug of the protease inhibitor amprenavir |
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| nitazoxanide | a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug; structure given in first source. It was investigated as a potential treatment for COVID-19 based on its broad antiviral activity, including in vitro activity against SARS-CoV-2 and MERS-CoV; however, there are no data to support the use of nitazoxanide in the treatment of COVID-19. |
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| ramipril | A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat. |
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| oseltamivir | Oseltamivir phosphate is an ethyl ester prodrug requiring ester hydrolysis for conversion to the active form, oseltamivir carboxylate. Oseltamivir carboxylate is an inhibitor of influenza virus neuraminidase affecting release of viral particles. The median IC50 values of oseltamivir against influenza A/H1N1, influenza A/H3N2, and influenza B clinical isolates were 2.5 nM (range 0.93-4.16 nM, N=74), 0.96 nM (range 0.13 - 7.95 nM, N=774), and 60 nM (20-285 nM, N=256), respectively, in a neuraminidase assay with a fluorescently labeled MUNANA substrate. Although oseltamivir was suggested as a potential treatment and included in various antiviral regimens used during the early stages of the COVID-19 pandemic, the drug does not appear to have in vitro activity against SARS-CoV-2 and there are no data to support the use of oseltamivir or other neuraminidase inhibitors in the treatment of COVID-19. |
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| baloxavir marboxil | Baloxavir marboxil is a prodrug that is converted by hydrolysis to baloxavir, the active form that exerts anti-influenza virus activity. Baloxavir inhibits the endonuclease activity of the polymerase acidic (PA) protein, an influenza virus-specific enzyme in the viral RNA polymerase complex required for viral gene transcription, resulting in inhibition of influenza virus replication. The 50% inhibitory concentration (IC50) of baloxavir was 1.4 to 3.1 nM (n=4) for influenza A viruses and 4.5 to 8.9 nM (n=3) for influenza B viruses in a PA endonuclease assay. Viruses with reduced susceptibility to baloxavir have amino acid substitutions in the PA protein. It was investigated as a potential treatment during the early stages of the COVID-19 pandemic but in vitro antiviral activity against SARS-CoV-2 was not confirmed. |
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| methylprednisolone suleptanate | prodrug of methylprednisolone |
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| isavuconazonium | prodrug of BAL4815 |
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