A SARS-CoV-2-specific CAR-T-cell model identifies felodipine, fasudil, imatinib, and caspofungin as potential treatments for lethal COVID-19
Cell Mol Immunol. 2023 Mar 2:1-14. doi: 10.1038/s41423-023-00985-3. Online ahead of print.ABSTRACTSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2)-induced cytokine storm is closely associated with coronavirus disease 2019 (COVID-19) severity and lethality. However, drugs that are effective against inflammation to treat lethal COVID-19 are still urgently needed. Here, we constructed a SARS-CoV-2 spike protein-specific CAR, and human T cells infected with this CAR (SARS-CoV-2-S CAR-T) and stimulated with spike protein mimicked the T-cell responses seen in COVID-19 patients, causing cytokine storm and displaying a...
Source: Cellular and Molecular Immunology - March 2, 2023 Category: Molecular Biology Authors: Lin Xia Lun-Zhi Yuan Ya-Hong Hu Jun-Yi Liu Guo-Sheng Hu Ruo-Yao Qi Tian-Ying Zhang Hua-Long Xiong Zao-Zao Zheng Hong-Wei Lin Jia-Mo Zhang Chao Yu Ming Zhou Jian Ma Tong Cheng Ri-Rong Chen Yi Guan Ning-Shao Xia Wen Liu Source Type: research

A SARS-CoV-2-specific CAR-T-cell model identifies felodipine, fasudil, imatinib, and caspofungin as potential treatments for lethal COVID-19
Cell Mol Immunol. 2023 Mar 2:1-14. doi: 10.1038/s41423-023-00985-3. Online ahead of print.ABSTRACTSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2)-induced cytokine storm is closely associated with coronavirus disease 2019 (COVID-19) severity and lethality. However, drugs that are effective against inflammation to treat lethal COVID-19 are still urgently needed. Here, we constructed a SARS-CoV-2 spike protein-specific CAR, and human T cells infected with this CAR (SARS-CoV-2-S CAR-T) and stimulated with spike protein mimicked the T-cell responses seen in COVID-19 patients, causing cytokine storm and displaying a...
Source: Cellular and Molecular Immunology - March 2, 2023 Category: Molecular Biology Authors: Lin Xia Lun-Zhi Yuan Ya-Hong Hu Jun-Yi Liu Guo-Sheng Hu Ruo-Yao Qi Tian-Ying Zhang Hua-Long Xiong Zao-Zao Zheng Hong-Wei Lin Jia-Mo Zhang Chao Yu Ming Zhou Jian Ma Tong Cheng Ri-Rong Chen Yi Guan Ning-Shao Xia Wen Liu Source Type: research

Physiologically Based Pharmacokinetic Modeling for Development and Applications of a Virtual Celiac Disease Population using Felodipine as a model drug
AbstractIn celiac disease (CeD) gastrointestinal CYP3A4 abundance and morphology is affected by the severity of disease. Therefore, exposure to CYP3A4 substrates and extent of drug interactions is altered. A PBPK population for different severities of CeD was developed. Gastrointestinal physiology parameters such as luminal pH, transit times, morphology, P-gp and CYP3A4 expression were included in development of the CeD population. Data on physiological difference between healthy and CeD subjects were incorporated into the model as the ratio of celiac to healthy. A PBPK model was developed and verified for felodipine exten...
Source: CPT: Pharmacometrics and Systems Pharmacology - March 1, 2023 Category: Drugs & Pharmacology Authors: Farzaneh Salem, Ali Nimavardi, Jennypher Mudunuru, Debra Tompson, Jackie Bloomer, David B. Turner, Kunal S. Taskar Tags: ARTICLE Source Type: research

[ASAP] Inhomogeneous Phase Significantly Reduces Oral Bioavailability of Felodipine/PVPVA Amorphous Solid Dispersion
Molecular PharmaceuticsDOI: 10.1021/acs.molpharmaceut.2c00695 (Source: Molecular Pharmaceutics)
Source: Molecular Pharmaceutics - December 19, 2022 Category: Drugs & Pharmacology Authors: Di Gao, Dan Zhu, Xue Zhou, Shuai Dong, and Yuejie Chen Source Type: research

A Mysterious Case of Abdominal Pain
Question: A 43-year-old woman with a history of hypertension and cholecystectomy presented with worsening epigastric pain associated with postprandial nausea and vomiting for the past few weeks. She denied recent travel, atopy, or new dietary or medication changes. She reports similar yearly episodes starting 15 years ago, lasting for a few weeks and resolving spontaneously. Medications consisted of lisinopril and felodipine. Vital signs were within normal range. Physical examination revealed epigastric tenderness. (Source: Gastroenterology)
Source: Gastroenterology - October 19, 2022 Category: Gastroenterology Authors: Abbinaya Elangovan, Dawn Zacharias, Fady G. Haddad Tags: Electronic Curbside Consult Source Type: research

Phytochemicals That Interfere With Drug Metabolism and Transport, Modifying Plasma Concentration in Humans and Animals
Dose Response. 2022 Sep 21;20(3):15593258221120485. doi: 10.1177/15593258221120485. eCollection 2022 Jul-Sep.ABSTRACTPhytochemicals (Pch) present in fruits, vegetables and other foods, are known to inhibit or induce drug metabolism and transport. An exhaustive search was performed in five databases covering from 2000 to 2021. Twenty-one compounds from plants were found to modulate CYP3A and/or P-gp activities and modified the pharmacokinetics and the therapeutic effect of 27 different drugs. Flavonols, flavanones, flavones, stilbenes, diferuloylmethanes, tannins, protoalkaloids, flavans, hyperforin and terpenes, reduce pla...
Source: Dose Response - September 26, 2022 Category: Drugs & Pharmacology Authors: Josefina G ómez-Garduño Renato Le ón-Rodríguez Radam és Alemón-Medina Beatriz E P érez-Guillé Rosa E Soriano-Rosales Ailema Gonz ález-Ortiz Juan L Ch ávez-Pacheco Edelmira Solorio-L ópez Paola Fernandez-P érez Liliana Rivera-Espinosa Source Type: research

Phytochemicals That Interfere With Drug Metabolism and Transport, Modifying Plasma Concentration in Humans and Animals
Dose Response. 2022 Sep 21;20(3):15593258221120485. doi: 10.1177/15593258221120485. eCollection 2022 Jul-Sep.ABSTRACTPhytochemicals (Pch) present in fruits, vegetables and other foods, are known to inhibit or induce drug metabolism and transport. An exhaustive search was performed in five databases covering from 2000 to 2021. Twenty-one compounds from plants were found to modulate CYP3A and/or P-gp activities and modified the pharmacokinetics and the therapeutic effect of 27 different drugs. Flavonols, flavanones, flavones, stilbenes, diferuloylmethanes, tannins, protoalkaloids, flavans, hyperforin and terpenes, reduce pla...
Source: Dose Response - September 26, 2022 Category: Drugs & Pharmacology Authors: Josefina G ómez-Garduño Renato Le ón-Rodríguez Radam és Alemón-Medina Beatriz E P érez-Guillé Rosa E Soriano-Rosales Ailema Gonz ález-Ortiz Juan L Ch ávez-Pacheco Edelmira Solorio-L ópez Paola Fernandez-P érez Liliana Rivera-Espinosa Source Type: research

Phytochemicals That Interfere With Drug Metabolism and Transport, Modifying Plasma Concentration in Humans and Animals
Dose Response. 2022 Sep 21;20(3):15593258221120485. doi: 10.1177/15593258221120485. eCollection 2022 Jul-Sep.ABSTRACTPhytochemicals (Pch) present in fruits, vegetables and other foods, are known to inhibit or induce drug metabolism and transport. An exhaustive search was performed in five databases covering from 2000 to 2021. Twenty-one compounds from plants were found to modulate CYP3A and/or P-gp activities and modified the pharmacokinetics and the therapeutic effect of 27 different drugs. Flavonols, flavanones, flavones, stilbenes, diferuloylmethanes, tannins, protoalkaloids, flavans, hyperforin and terpenes, reduce pla...
Source: Dose Response - September 26, 2022 Category: Drugs & Pharmacology Authors: Josefina G ómez-Garduño Renato Le ón-Rodríguez Radam és Alemón-Medina Beatriz E P érez-Guillé Rosa E Soriano-Rosales Ailema Gonz ález-Ortiz Juan L Ch ávez-Pacheco Edelmira Solorio-L ópez Paola Fernandez-P érez Liliana Rivera-Espinosa Source Type: research

Inhibitory effect of 20(S)-protopanaxadiol on cytochrome P450: Potential of its pharmacokinetic interactions in vivo
In conclusion, 20(S)-PPD likely affects the in vivo metabolism of CYP3A4 or CYP2B6 substrates, suggesting a need for careful attention when concomitantly administering 20(S)-PPD with other medications. This study will broaden our understanding of ginseng and products containing precursor ginsenosides of 20(S)-PPD for safer and more efficient use in humans.PMID:36076601 | DOI:10.1016/j.biopha.2022.113514 (Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie)
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - September 9, 2022 Category: Drugs & Pharmacology Authors: Su Gwon Lee Kwan Hyung Cho Thi-Thao-Linh Nguyen Dang-Khoa Vo Yoon-Jee Chae Han-Joo Maeng Source Type: research

Dihydropyridine-derived calcium channel blocker as a promising anti-hantavirus entry inhibitor
In this study, we discovered that benidipine hydrochloride, a calcium channel blocker, inhibits the entry of hantaviruses in vitro. Moreover, an array of calcium channel inhibitors, such as cilnidipine, felodipine, amlodipine, manidipine, nicardipine, and nisoldipine, exhibit similar antiviral properties. Using pseudotyped vesicular stomatitis viruses harboring the different hantavirus glycoproteins, we demonstrate that benidipine hydrochloride inhibits the infection by both HFRS- and HPS-causing hantaviruses. The results of our study indicate the possibility of repurposing FDA-approved calcium channel blockers for the tre...
Source: Frontiers in Pharmacology - August 29, 2022 Category: Drugs & Pharmacology Source Type: research

Felodipine
(Source: Reactions Weekly)
Source: Reactions Weekly - August 1, 2022 Category: Drugs & Pharmacology Source Type: research

[ASAP] Water-Resistant Drug –Polymer Interaction Contributes to the Formation of Nano-Species during the Dissolution of Felodipine Amorphous Solid Dispersions
Molecular PharmaceuticsDOI: 10.1021/acs.molpharmaceut.2c00250 (Source: Molecular Pharmaceutics)
Source: Molecular Pharmaceutics - June 27, 2022 Category: Drugs & Pharmacology Authors: Lei Liu, Linc Chen, Wouter Mu ̈llers, Peter Serno, and Feng Qian Source Type: research

Development of a Microgram Scale Video-Microscopic Method to Investigate Dissolution Behavior of Poorly Water-Soluble Drugs
AAPS PharmSciTech. 2022 Jun 24;23(6):173. doi: 10.1208/s12249-022-02322-9.ABSTRACTPoor aqueous solubility is a common characteristic of new drug candidates, which leads to low or inconsistent oral bioavailability. This has sparked an interest in material efficient testing of solubility and dissolution rate. The aim was to develop a microgram scale video-microscopic method to screen the dissolution rates of poorly water-soluble drugs. This method was applied to six drugs (carvedilol, diazepam, dipyridamole, felodipine, fenofibrate, and indomethacin) in fasted state simulated intestinal fluid (FaSSIF), of indomethacin in buf...
Source: AAPS PharmSciTech - June 23, 2022 Category: Drugs & Pharmacology Authors: Malte B øgh Senniksen Juliane Fjelrad Christfort Riccardo Marabini Erik Spillum Wayne Matthews Luigi Da Vi à Jakob Plum Thomas Rades Anette M üllertz Source Type: research

Development of a Microgram Scale Video-Microscopic Method to Investigate Dissolution Behavior of Poorly Water-Soluble Drugs
AAPS PharmSciTech. 2022 Jun 24;23(6):173. doi: 10.1208/s12249-022-02322-9.ABSTRACTPoor aqueous solubility is a common characteristic of new drug candidates, which leads to low or inconsistent oral bioavailability. This has sparked an interest in material efficient testing of solubility and dissolution rate. The aim was to develop a microgram scale video-microscopic method to screen the dissolution rates of poorly water-soluble drugs. This method was applied to six drugs (carvedilol, diazepam, dipyridamole, felodipine, fenofibrate, and indomethacin) in fasted state simulated intestinal fluid (FaSSIF), of indomethacin in buf...
Source: AAPS PharmSciTech - June 23, 2022 Category: Drugs & Pharmacology Authors: Malte B øgh Senniksen Juliane Fjelrad Christfort Riccardo Marabini Erik Spillum Wayne Matthews Luigi Da Vi à Jakob Plum Thomas Rades Anette M üllertz Source Type: research