Lineage of drug discovery research on fluorinated pyrimidines: chronicle of the achievements accomplished by Professor Setsuro Fujii
Int J Clin Oncol. 2023 Mar 24. doi: 10.1007/s10147-023-02326-w. Online ahead of print.ABSTRACTProf. Setsuro Fujii achieved significant results in the field of drug discovery research in Japan. He developed nine well-known drugs: FT, UFT, S-1 and FTD/TPI are anticancer drugs, while cetraxate hydrochloride, camostat mesilate, nafamostat mesilate, gabexate mesilate and pravastatin sodium are therapeutic drugs for various other diseases. He delivered hope to patients with various diseases across the world to improve their condition. Even now, drug discovery research based on Dr. Fujii's ideas is continuing.PMID:36961615 | DOI:...
Source: Clinical Breast Cancer - March 24, 2023 Category: Cancer & Oncology Authors: Yoshihiko Maehara Eiji Oki Mitsuhiko Ota Norifumi Harimoto Koji Ando Ryota Nakanishi Tetsuro Kawazoe Yoshiaki Fujimoto Kentaro Nonaka Hiroyuki Kitao Makoto Iimori Kunio Makino Teiji Takechi Takeshi Sagara Kazutaka Miyadera Kazuaki Matsuoka Hiroshi Tsukiha Source Type: research

Lineage of drug discovery research on fluorinated pyrimidines: chronicle of the achievements accomplished by Professor Setsuro Fujii
Int J Clin Oncol. 2023 Mar 24. doi: 10.1007/s10147-023-02326-w. Online ahead of print.ABSTRACTProf. Setsuro Fujii achieved significant results in the field of drug discovery research in Japan. He developed nine well-known drugs: FT, UFT, S-1 and FTD/TPI are anticancer drugs, while cetraxate hydrochloride, camostat mesilate, nafamostat mesilate, gabexate mesilate and pravastatin sodium are therapeutic drugs for various other diseases. He delivered hope to patients with various diseases across the world to improve their condition. Even now, drug discovery research based on Dr. Fujii's ideas is continuing.PMID:36961615 | DOI:...
Source: Clinical Genitourinary Cancer - March 24, 2023 Category: Cancer & Oncology Authors: Yoshihiko Maehara Eiji Oki Mitsuhiko Ota Norifumi Harimoto Koji Ando Ryota Nakanishi Tetsuro Kawazoe Yoshiaki Fujimoto Kentaro Nonaka Hiroyuki Kitao Makoto Iimori Kunio Makino Teiji Takechi Takeshi Sagara Kazutaka Miyadera Kazuaki Matsuoka Hiroshi Tsukiha Source Type: research

Lineage of drug discovery research on fluorinated pyrimidines: chronicle of the achievements accomplished by Professor Setsuro Fujii
AbstractProf. Setsuro Fujii achieved significant results in the field of drug discovery research in Japan. He developed nine well-known drugs: FT, UFT, S-1 and FTD/TPI are anticancer drugs, while cetraxate hydrochloride, camostat mesilate, nafamostat mesilate, gabexate mesilate and pravastatin sodium are therapeutic drugs for various other diseases. He delivered hope to patients with various diseases across the world to improve their condition. Even now, drug discovery research based on Dr. Fujii ’s ideas is continuing. (Source: International Journal of Clinical Oncology)
Source: International Journal of Clinical Oncology - March 24, 2023 Category: Cancer & Oncology Source Type: research

Plasma Progerin in Patients With Hutchinson-Gilford Progeria Syndrome: Immunoassay Development and Clinical Evaluation
CONCLUSIONS: A sensitive, quantitative immunoassay for progerin was developed and used to demonstrate high progerin levels in HGPS plasma that decreased with lonafarnib therapy. The extent of improved survival was associated with both the magnitude of progerin decrease and duration at lower levels. Thus, plasma progerin is a biomarker for HGPS whose reduction enables short- and long-term assessment of progerin-targeted treatment efficacy.REGISTRATION: URL: https://www.CLINICALTRIALS: gov. Unique identifiers: NCT00879034 and NCT00916747.PMID:36919608 | DOI:10.1161/CIRCULATIONAHA.122.060002 (Source: Atherosclerosis)
Source: Atherosclerosis - March 15, 2023 Category: Cardiology Authors: Leslie B Gordon Wendy Norris Sarah Hamren Robert Goodson Jessica LeClair Joseph Massaro Asya Lyass Ralph B D'Agostino Kelsey Tuminelli Mark W Kieran Monica E Kleinman Source Type: research

Plasma Progerin in Patients With Hutchinson-Gilford Progeria Syndrome: Immunoassay Development and Clinical Evaluation
CONCLUSIONS: A sensitive, quantitative immunoassay for progerin was developed and used to demonstrate high progerin levels in HGPS plasma that decreased with lonafarnib therapy. The extent of improved survival was associated with both the magnitude of progerin decrease and duration at lower levels. Thus, plasma progerin is a biomarker for HGPS whose reduction enables short- and long-term assessment of progerin-targeted treatment efficacy.REGISTRATION: URL: https://www.CLINICALTRIALS: gov. Unique identifiers: NCT00879034 and NCT00916747.PMID:36919608 | DOI:10.1161/CIRCULATIONAHA.122.060002 (Source: Circulation)
Source: Circulation - March 15, 2023 Category: Cardiology Authors: Leslie B Gordon Wendy Norris Sarah Hamren Robert Goodson Jessica LeClair Joseph Massaro Asya Lyass Ralph B D'Agostino Kelsey Tuminelli Mark W Kieran Monica E Kleinman Source Type: research

Plasma Progerin in Patients With Hutchinson-Gilford Progeria Syndrome: Immunoassay Development and Clinical Evaluation
CONCLUSIONS: A sensitive, quantitative immunoassay for progerin was developed and used to demonstrate high progerin levels in HGPS plasma that decreased with lonafarnib therapy. The extent of improved survival was associated with both the magnitude of progerin decrease and duration at lower levels. Thus, plasma progerin is a biomarker for HGPS whose reduction enables short- and long-term assessment of progerin-targeted treatment efficacy.REGISTRATION: URL: https://www.CLINICALTRIALS: gov. Unique identifiers: NCT00879034 and NCT00916747.PMID:36919608 | DOI:10.1161/CIRCULATIONAHA.122.060002 (Source: Atherosclerosis)
Source: Atherosclerosis - March 15, 2023 Category: Cardiology Authors: Leslie B Gordon Wendy Norris Sarah Hamren Robert Goodson Jessica LeClair Joseph Massaro Asya Lyass Ralph B D'Agostino Kelsey Tuminelli Mark W Kieran Monica E Kleinman Source Type: research

Plasma Progerin in Patients With Hutchinson-Gilford Progeria Syndrome: Immunoassay Development and Clinical Evaluation
CONCLUSIONS: A sensitive, quantitative immunoassay for progerin was developed and used to demonstrate high progerin levels in HGPS plasma that decreased with lonafarnib therapy. The extent of improved survival was associated with both the magnitude of progerin decrease and duration at lower levels. Thus, plasma progerin is a biomarker for HGPS whose reduction enables short- and long-term assessment of progerin-targeted treatment efficacy.REGISTRATION: URL: https://www.CLINICALTRIALS: gov. Unique identifiers: NCT00879034 and NCT00916747.PMID:36919608 | DOI:10.1161/CIRCULATIONAHA.122.060002 (Source: Circulation)
Source: Circulation - March 15, 2023 Category: Cardiology Authors: Leslie B Gordon Wendy Norris Sarah Hamren Robert Goodson Jessica LeClair Joseph Massaro Asya Lyass Ralph B D'Agostino Kelsey Tuminelli Mark W Kieran Monica E Kleinman Source Type: research

Organic anion-transporting polypeptide 2B1 knockout and humanized mice; insights into the handling of bilirubin and drugs
Pharmacol Res. 2023 Mar 10:106724. doi: 10.1016/j.phrs.2023.106724. Online ahead of print.ABSTRACTOrganic anion transporting polypeptide 2B1 (OATP2B1/SLCO2B1) facilitates uptake transport of structurally diverse endogenous and exogenous compounds. To investigate the roles of OATP2B1 in physiology and pharmacology, we established and characterized Oatp2b1 knockout (single Slco2b1-/- and combination Slco1a/1b/2b1-/-) and humanized hepatic and intestinal OATP2B1 transgenic mouse models. While viable and fertile, these strains exhibited a modestly increased body weight. In males, unconjugated bilirubin levels were markedly red...
Source: Cancer Control - March 12, 2023 Category: Cancer & Oncology Authors: Wenlong Li Dilek Iusuf Rolf W Sparidans Els Wagenaar Yaogeng Wang Dirk R de Waart Margarida L F Martins St éphanie van Hoppe Maria C Lebre Olaf van Tellingen Jos H Beijnen Alfred H Schinkel Source Type: research

Evaluation of the Potential for Cytochrome P450 and Transporter-Mediated Drug-Drug Interactions for Cilofexor, a Selective Nonsteroidal Farnesoid X Receptor (FXR) Agonist
ConclusionCilofexor may be coadministered with inhibitors of P-gp, CYP3A4, or CYP2C8 without the need for dose modification. Cilofexor may be coadministered with OATP, BCRP, P-gp, and/or CYP3A4 substrates —including statins—without dose modification. However, coadministration of cilofexor with strong hepatic OATP inhibitors, or with strong or moderate inducers of OATP/CYP2C8, is not recommended. (Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - March 11, 2023 Category: Drugs & Pharmacology Source Type: research

Neuroprotective effects of pravastatin in cerebral venous infarction in a rat model
CONCLUSIONS: Pre-emptive administration of pravastatin sodium mixed in the food has neuroprotective effects against cerebral cortical venous ischemia with suppression of apoptosis associated with inhibition of Bax expression but has little influence on regional CBF.PMID:36852215 | PMC:PMC9958423 | DOI:10.1016/j.ibneur.2023.02.002 (Source: Atherosclerosis)
Source: Atherosclerosis - February 28, 2023 Category: Cardiology Authors: Fumiya Sato Daisuke Wajima Yasuhiro Takeshima Ichiro Nakagawa Taekyun Kim Yasushi Motoyama Young-Soo Park Hiroyuki Nakase Source Type: research

Does aspirin have a place in primary cardiovascular prevention by the polypill  ? Simulation study on a realistic virtual population
CONCLUSION: Until proven otherwise, aspirin has only a limited place in individuals between 35 and 65 years without a cardiovascular history. We showed how simulating therapeutic strategies on a realistic virtual population could be used for best applying available evidence.PMID:36841655 | DOI:10.1016/j.therap.2023.01.011 (Source: Therapie)
Source: Therapie - February 25, 2023 Category: Psychiatry & Psychology Authors: Mor Fall Guillaume Grenet Hai-Ha Le Behrouz Kassa ï Jean-Christophe Lega R émy Boussageon Sabine Mainbourg Ivanny Marchant Johanne Gafsi Amadou Moctar Dieye Fran çois Gueyffier Source Type: research

Does aspirin have a place in primary cardiovascular prevention by the polypill  ? Simulation study on a realistic virtual population
CONCLUSION: Until proven otherwise, aspirin has only a limited place in individuals between 35 and 65 years without a cardiovascular history. We showed how simulating therapeutic strategies on a realistic virtual population could be used for best applying available evidence.PMID:36841655 | DOI:10.1016/j.therap.2023.01.011 (Source: Therapie)
Source: Therapie - February 25, 2023 Category: Psychiatry & Psychology Authors: Mor Fall Guillaume Grenet Hai-Ha Le Behrouz Kassa ï Jean-Christophe Lega R émy Boussageon Sabine Mainbourg Ivanny Marchant Johanne Gafsi Amadou Moctar Dieye Fran çois Gueyffier Source Type: research

Long-Term Neurodevelopmental Follow-up of Children Exposed to Pravastatin in-Utero
Preeclampsia, especially when preterm, increases risk of child neurodevelopmental adverse outcomes. Biological plausibility, preclinical studies, and pilot clinical trials conducted by the Eunice Kennedy Shriver National Institute of Child Health and Human Development-Obstetrics Fetal Pharmacology Research Centers Network support the safety and utility of pravastatin to prevent preeclampsia. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - February 24, 2023 Category: OBGYN Authors: Maged M. Costantine, Rebecca G. Clifton, Trisha M. Boekhoudt, Kirsten Lawrence, Cynthia Gyamfi-Bannerman, Katherine L. Wisner, William Grobman, Steve N. Caritis, Hyagriv N. Simhan, Mary F. Hebert, Monica Longo, George R. Saade, Eunice Kennedy Shriver Nati Tags: Original Research: Obstetrics Source Type: research

Long-term neurodevelopmental follow-up of children exposed to pravastatin in utero
Preeclampsia, especially before term, increases the risk of child neurodevelopmental adverse outcomes. Biological plausibility, preclinical studies, and pilot clinical trials conducted by the Eunice Kennedy Shriver National Institute of Child Health and Human Development and the Obstetric-Fetal Pharmacology Research Centers Network support the safety and use of pravastatin to prevent preeclampsia. (Source: American Journal of Obstetrics and Gynecology)
Source: American Journal of Obstetrics and Gynecology - February 24, 2023 Category: OBGYN Authors: Maged M. Costantine, Rebecca G. Clifton, Trisha M. Boekhoudt, Kirsten Lawrence, Cynthia Gyamfi-Bannerman, Katherine L. Wisner, William Grobman, Steve N. Caritis, Hyagriv N. Simhan, Mary F. Hebert, Monica Longo, George R. Saade, Eunice Kennedy Shriver Nati Tags: Original Research Source Type: research