The likely first step is binding of the prodrug protonated on the pyridine of the compound with cysteine 813. Then the second ... Proton pump inhibitors are prodrugs and their actual inhibitory form is somewhat controversial. In acidic solution, the ... 414-5. Hemenway, Jeffrey N. (2007). "Case Study: Omeprazole (Prilosec)". Prodrugs. Biotechnology: Pharmaceutical Aspects. pp. ...
414-5. Hemenway JN (2007). "Case Study: Omeprazole (Prilosec)". Prodrugs. Biotechnology: Pharmaceutical Aspects. pp. 1313-21. ...
263-. ISBN 978-3-642-60107-1. Aungst, Bruce J.; Matz, Nicole (2007). "Prodrugs to Reduce Presystemic Metabolism". Prodrugs. ... It is a prodrug of estradiol and appears to be partially protected from first-pass metabolism in the liver and intestines with ... Patel JU, Prankerd RJ, Sloan KB (October 1994). "A prodrug approach to increasing the oral potency of a phenolic drug. 1. ... "A prodrug approach to increasing the oral potency of a phenolic drug. Part 2. Pharmacodynamics and preliminary bioavailability ...
In the case of a dendrimer prodrug structure, linking of a drug to a dendrimer may be direct or linker-mediated depending on ... da Silva Santos S, Igne Ferreira E, Giarolla J (May 2016). "Dendrimer Prodrugs". Molecules. 21 (6): 686. doi:10.3390/ ... a covalent attachment or conjugation to the external surface of the dendrimer forming a dendrimer prodrug, (2) ionic ...
The medication is a prodrug of norethisterone in the body, with etynodiol occurring as an intermediate. Etynodiol, a related ... 216-. ISBN 978-1-4832-7738-7. Hammerstein J (1990). "Prodrugs: advantage or disadvantage?". Am. J. Obstet. Gynecol. 163 (6 Pt 2 ... is virtually inactive in terms of affinity for the progesterone and androgen receptors and acts as a rapidly converted prodrug ...
It is a prodrug of various active metabolites in the body, such as norethisterone among others. Noretynodrel was introduced for ... It is considered to be a prodrug, and for this reason, the metabolites of noretynodrel play an important role in its biological ... Hammerstein J (1990). "Prodrugs: advantage or disadvantage?". Am. J. Obstet. Gynecol. 163 (6 Pt 2): 2198-203. doi:10.1016/0002- ... Tibolone is considered to be a prodrug of both its 3α- and 3β-hydroxylated and δ4-isomerized metabolites. Noretynodrel is also ...
Ahmed G, Elger W, Meece F, Nair HB, Schneider B, Wyrwa R, Nickisch K (October 2017). "A prodrug design for improved oral ... Esterification is useful because it is often able to render the parent steroid into a prodrug of itself with altered chemical ... Like many other steroid esters, they are prodrugs. Unlike other steroid esters however, they bypass first-pass metabolism with ... Valentino Stella; Ronald Borchardt; Michael Hageman; Reza Oliyai, Hans Maag, Jefferson Tilley (12 March 2007). Prodrugs: ...
Stella, V. (1975). "Pro-drugs: An Overview and Definition". Pro-drugs as Novel Drug Delivery Systems. ACS Symposium Series. 14 ... Wermuth, Camille G. (2008). "Designing Prodrugs and Bioprecursors". The Practice of Medicinal Chemistry. pp. 721-746. doi: ...
These are called prodrugs. The reasons for this type of formulation may be because the drug is more stable during manufacture ... Müller CE (November 2009). "Prodrug approaches for enhancing the bioavailability of drugs with low solubility". Chemistry & ... and storage as the prodrug form, or because the prodrug is better absorbed by the body or has superior pharmacokinetics (e.g., ...
CS1 maint: discouraged parameter (link) Maddox, Gary (17 August 2009). "A pro-drugs movie? Get off the grass, says director". ...
It is the C21 pivalate (trimethylacetate) ester of clocortolone, and acts as a prodrug of clocortolone in the body. Elks J (14 ... 79-. ISBN 978-94-011-4439-1. US 5073641, Bundgaard H, Nielsen NM, "Prodrug derivatives of carboxylic acid drugs", issued 17 ... December 1991 Stella V, Borchardt R, Hageman M, Oliyai R, Maag H, Tilley J (12 March 2007). Prodrugs: Challenges and Rewards. ...
List of estrogen esters § Estradiol esters Hussain MA, Aungst BJ, Shefter E (January 1988). "Prodrugs for improved oral beta- ... 218-. ISBN 978-3-527-63318-0. Hansen, Joan; Mørk, Niels; Bundgaard, Hans (1992). "Phenyl carbamates of amino acids as prodrug ... 347-. ISBN 978-0-387-49785-3.CS1 maint: multiple names: authors list (link) Jarkko Rautio (11 January 2011). Prodrugs and ... "Oral bioavailability of 17β-estradiol and various ester prodrugs in the rat". International Journal of Pharmaceutics. 76 (1-2 ...
It is a prodrug, and upon oral administration, is rapidly and almost completely converted into norethisterone, a potent ... Hammerstein J (1990). "Prodrugs: advantage or disadvantage?". Am. J. Obstet. Gynecol. 163 (6 Pt 2): 2198-203. doi:10.1016/0002- ... The medication is a prodrug of norethisterone in the body, with etynodiol occurring as an intermediate. Lynestrenol was ...
Noretynodrel may also be a prodrug of norethisterone. NETA is taken by mouth similarly to norethisterone, while NETE is given ... However, NETE, an intramuscularly administered prodrug of norethisterone which is used as a long-acting contraceptive, is used ... ISBN 978-0-323-00201-1. Hammerstein J (December 1990). "Prodrugs: advantage or disadvantage?". American Journal of Obstetrics ... Similar androgenic potential is inherent to norethisterone and its prodrugs (norethisterone acetate, ethynodiol diacetate, ...
List of estrogen esters § Estradiol esters Hussain MA, Aungst BJ, Shefter E (January 1988). "Prodrugs for improved oral beta- ... Prodrugs: Challenges and Rewards. Springer Science & Business Media. pp. 347-. ISBN 978-0-387-49785-3.CS1 maint: multiple names ... authors list (link) Hansen, Joan; Mørk, Niels; Bundgaard, Hans (1992). "Phenyl carbamates of amino acids as prodrug forms for ... "Oral bioavailability of 17β-estradiol and various ester prodrugs in the rat". International Journal of Pharmaceutics. 76 (1-2 ...
The drug is a phosphate ester and prodrug of miproxifene (DP-TAT-59) with improved water solubility that was better suited for ... Stella V, Borchardt R, Hageman M, Oliyai R, Maag H, Tilley J (12 March 2007). Prodrugs: Challenges and Rewards. Springer ...
It is a prodrug of estramustine and estromustine in terms of its cytostatic effects and a prodrug of estradiol in relation to ... In terms of its pharmacodynamic effects, EMP is a prodrug of estramustine, estromustine, and estradiol. As a prodrug of ... Because EMP is a prodrug of estradiol, it may be considered to be a natural and bioidentical form of estrogen, although it does ... EMP was originally developed as a dual ester prodrug of an estrogen and normustine as a nitrogen mustard alkylating ...
Prodrugs: Challenges and Rewards. Springer Science & Business Media. p. 58. ISBN 978-0-387-49782-2.CS1 maint: multiple names: ... "Estradiol prodrugs (EP) for efficient oral estrogen treatment and abolished effects on estrogen modulated liver functions". J. ... "Sulfamates of various estrogens are prodrugs with increased systemic and reduced hepatic estrogenicity at oral application". J ...
Valentino Stella; Ronald Borchardt; Michael Hageman; Reza Oliyai, Hans Maag, Jefferson Tilley (26 August 2007). Prodrugs: ... DHTU is a prodrug of DHT. Similarly to testosterone undecanoate (TU), DHTU is orally active. It occurs as an important active ...
... is a prodrug of norethisterone, and is converted immediately and completely into norethisterone. Etynodiol is an ... 146-. ISBN 978-92-832-1291-1. Hammerstein J (December 1990). "Prodrugs: advantage or disadvantage?". American Journal of ... intermediate in the conversion of the prodrug lynestrenol into norethisterone. Etynodiol is a 19-nortestosterone derivative. ...
Stella V, Borchardt R, Hageman M, Oliyai R, Maag H, Tilley J (12 March 2007). Prodrugs: Challenges and Rewards. Springer ... Miproxifene is the active metabolite of miproxifene phosphate (TAT-59), a phosphate ester and prodrug of miproxifene that was ...
It is a prodrug of epitiostanol. The drug was patented and described in 1968. Mepitiostane is used as an antiestrogen and ... Prodrugs: Challenges and Rewards. Springer Science & Business Media. pp. 660-. ISBN 978-0-387-49782-2. Ronald T. Borchardt; ...
... also activates some prodrugs. This enzyme also metabolizes several endogenous substances, such as hydroxytryptamines, ...
Once in the cells, the prodrug was enzymatically converted into the active, toxic form. The first clinical trials were ... They converted the base nitrogen mustard into a nontoxic "transport form". This transport form was a prodrug, subsequently ... Huttunen KM, Raunio H, Rautio J (September 2011). "Prodrugs--from serendipity to rational design". Pharmacological Reviews. 63 ...
Certain pro-drugs of GABA (ex. picamilon) have been developed to permeate the blood-brain barrier, then separate into GABA and ... Prodrugs allow for a direct increase of GABA levels throughout all areas of the brain, in a manner following the distribution ... GABAergic pro-drugs include chloral hydrate, which is metabolised to trichloroethanol, which then acts via the GABAA receptor. ... pattern of the pro-drug prior to metabolism.[citation needed] GABA enhanced the catabolism of serotonin into N-acetylserotonin ...
These drugs act as pro-drugs, which in themselves are not toxic, but are converted to toxic drugs by phosphorylation by viral ... Human thymidine kinase, in contrast, with its more narrow specificity, is unable to phosphorylate and activate the prodrug. In ... July 2015). "Synergistic effects of co-administration of suicide gene expressing mesenchymal stem cells and prodrug- ... Weinschenk L, Schols D, Balzarini J, Meier C (August 2015). "Nucleoside Diphosphate Prodrugs: Nonsymmetric DiPPro-Nucleotides ...
Although esters of steroidal androgens and estrogens are generally inactive themselves and act as prodrugs, the same is not ... Many (though not all) steroid esters function as prodrugs. Esterification is particularly salient in the case of progesterone ... Although it was originally thought that progesterone ethers like quingestrone were prodrugs of progesterone, it was ... Charman, William N.; Porter, Christopher J.H. (1996). "Lipophilic prodrugs designed for intestinal lymphatic transport". ...
Ahmed G, Elger W, Meece F, Nair HB, Schneider B, Wyrwa R, Nickisch K (October 2017). "A prodrug design for improved oral ... Patel J, Katovich MJ, Sloan KB, Curry SH, Prankerd RJ (February 1995). "A prodrug approach to increasing the oral potency of a ... This is a list of estrogen esters, or ester prodrugs of estrogens. It includes esters, as well as ethers, of steroidal ... ISBN 978-1-4757-2085-3. Patel JU, Prankerd RJ, Sloan KB (October 1994). "A prodrug approach to increasing the oral potency of a ...
Polymer-Directed Enzyme Prodrug Therapy (PDEPT) is an example of two-step anticancer treatment. Feng, Q; Tong, R (2016). " ... "drug Conjugates: Progress in Polymeric Prodrugs." ScienceDirect.com. Ernest Mario School of Pharmacy, n.d. Web. 12 Dec. 2012. ...
I don't think anyone who listens to Sorted would come away thinking it had a pro-drugs message. If they did I would say they ... Lead singer Jarvis Cocker released a statement two days later saying: "...'Sorted' is not a pro-drugs song... Nowhere on the ... "pro-drugs" and called for the single to be banned. The pre-release single had an inlay which Thornton alleged showed how to ...