Matches in SemOpenAlex for { <https://semopenalex.org/work/W4211212087> ?p ?o ?g. }
- W4211212087 endingPage "201" @default.
- W4211212087 startingPage "173" @default.
- W4211212087 abstract "Compound attrition continues to be a major burden that halts the progress and development of new molecular entities (NMEs). This chapter outlines the various factors that play a key role in the progress of NMEs with good hepatic stability and high oral bioavailability. It reviews known chemical space associated with metabolizing enzymes and discusses known approaches that can be used to increase metabolic stability for NMEs. The introduction of polarity is a key strategy that is considered to reduce hepatic metabolic clearance. Bioisosteric replacement of hydrogen using halogens has been considered since they can influence the physicochemical properties, biological activity, metabolism, pharmacokinetics, and pharmacodynamics of a molecule. This strategy is considered to improve the oral exposure of compounds that is attributed to high intestinal/hepatic first-pass effects. Nalbuphine is a potent opioid analgesic that is primarily metabolized by phenolic hydroxyl group conjugation that leads to significant first-pass effect and low oral bioavailability in preclinical species and humans." @default.
- W4211212087 created "2022-02-13" @default.
- W4211212087 date "2017-05-05" @default.
- W4211212087 modified "2023-10-16" @default.
- W4211212087 title "Physicochemical and Biopharmaceutical Factors Affecting Hepatic/Intestinal First‐Pass Effect" @default.
- W4211212087 cites W107008119 @default.
- W4211212087 cites W1877205841 @default.
- W4211212087 cites W1894357711 @default.
- W4211212087 cites W194358146 @default.
- W4211212087 cites W1964677552 @default.
- W4211212087 cites W1966437874 @default.
- W4211212087 cites W1968779484 @default.
- W4211212087 cites W1972416867 @default.
- W4211212087 cites W1976595875 @default.
- W4211212087 cites W1979097034 @default.
- W4211212087 cites W1979157320 @default.
- W4211212087 cites W1980242958 @default.
- W4211212087 cites W1982940569 @default.
- W4211212087 cites W1984845914 @default.
- W4211212087 cites W1985227921 @default.
- W4211212087 cites W1988137261 @default.
- W4211212087 cites W1989002205 @default.
- W4211212087 cites W1994438706 @default.
- W4211212087 cites W1995622516 @default.
- W4211212087 cites W1998356651 @default.
- W4211212087 cites W1998700502 @default.
- W4211212087 cites W2004170415 @default.
- W4211212087 cites W2004881900 @default.
- W4211212087 cites W2011559396 @default.
- W4211212087 cites W2011628325 @default.
- W4211212087 cites W2016029871 @default.
- W4211212087 cites W2017519065 @default.
- W4211212087 cites W2019925143 @default.
- W4211212087 cites W2020987809 @default.
- W4211212087 cites W2027179985 @default.
- W4211212087 cites W2027806414 @default.
- W4211212087 cites W2031343616 @default.
- W4211212087 cites W2032049376 @default.
- W4211212087 cites W2034590656 @default.
- W4211212087 cites W2034970387 @default.
- W4211212087 cites W2040978904 @default.
- W4211212087 cites W2043072338 @default.
- W4211212087 cites W2045178508 @default.
- W4211212087 cites W2047979347 @default.
- W4211212087 cites W2048267494 @default.
- W4211212087 cites W2049902803 @default.
- W4211212087 cites W2052659467 @default.
- W4211212087 cites W2054030734 @default.
- W4211212087 cites W2055988464 @default.
- W4211212087 cites W2063442560 @default.
- W4211212087 cites W2065918526 @default.
- W4211212087 cites W2065976317 @default.
- W4211212087 cites W2068473321 @default.
- W4211212087 cites W2068874904 @default.
- W4211212087 cites W2070685035 @default.
- W4211212087 cites W2072152260 @default.
- W4211212087 cites W2073073931 @default.
- W4211212087 cites W2076336531 @default.
- W4211212087 cites W2084086193 @default.
- W4211212087 cites W2085313140 @default.
- W4211212087 cites W2092136493 @default.
- W4211212087 cites W2095115792 @default.
- W4211212087 cites W2096500984 @default.
- W4211212087 cites W2097370520 @default.
- W4211212087 cites W2106715005 @default.
- W4211212087 cites W2107001433 @default.
- W4211212087 cites W2111668019 @default.
- W4211212087 cites W2112403717 @default.
- W4211212087 cites W2112634018 @default.
- W4211212087 cites W2118590909 @default.
- W4211212087 cites W2118664900 @default.
- W4211212087 cites W2119199557 @default.
- W4211212087 cites W2120152745 @default.
- W4211212087 cites W2121904963 @default.
- W4211212087 cites W2124945212 @default.
- W4211212087 cites W2125129553 @default.
- W4211212087 cites W2126901834 @default.
- W4211212087 cites W2127896256 @default.
- W4211212087 cites W2129701778 @default.
- W4211212087 cites W2140744815 @default.
- W4211212087 cites W2141755600 @default.
- W4211212087 cites W2145626389 @default.
- W4211212087 cites W2149415752 @default.
- W4211212087 cites W2150809120 @default.
- W4211212087 cites W2150946709 @default.
- W4211212087 cites W2157289463 @default.
- W4211212087 cites W2161976213 @default.
- W4211212087 cites W2162965277 @default.
- W4211212087 cites W2165417769 @default.
- W4211212087 cites W2166565533 @default.
- W4211212087 cites W2166960145 @default.
- W4211212087 cites W2171767046 @default.
- W4211212087 cites W2315921289 @default.
- W4211212087 cites W2317224907 @default.
- W4211212087 cites W2327180352 @default.
- W4211212087 cites W2503275033 @default.
- W4211212087 cites W2951646900 @default.
- W4211212087 cites W4236533258 @default.