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Hydroxychloroquine

Hydroxychloroquine prophylaxis and treatment is ineffective in macaque and hamster SARS-CoV-2 disease models

October 27, 2020 - 15:46 -- Open Access
Author(s): 
Rosenke K, Jarvis MA, Feldmann H, et al.
Reference: 
JCI Insight. 2020 Oct 22:143174

We remain largely without effective prophylactic/therapeutic interventions for COVID-19. Although many human COVID-19 clinical trials are ongoing, there remains a deficiency of supportive preclinical drug efficacy studies to help guide decisions. Here we assessed the prophylactic/therapeutic efficacy of hydroxychloroquine (HCQ), a drug of interest for COVID-19 management, in two animal disease models.

Finding the Dose for Hydroxychloroquine Prophylaxis for COVID-19: The Desperate Search for Effectiveness

October 7, 2020 - 16:11 -- Open Access
Author(s): 
Al-Kofahi M, Jacobson P, Boulware DR, Matas A, Kandaswamy R, Jaber MM, Rajasingham R, Young JH, Nicol MR
Reference: 
Clin Pharmacol Ther. 2020 Oct;108(4):766-769

Hydroxychloroquine is an antimalarial drug being tested as a potential treatment for the novel coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2. Although the efficacy of hydroxychloroquine for COVID-19 remains uncertain, it may serve as a potential prophylactic agent especially in those at high risk, such as healthcare workers, household contacts of infected patients, and the immunocompromised.

Brief Report: Hydroxychloroquine does not induce hemolytic anemia or organ damage in a "humanized" G6PD A- mouse model

October 6, 2020 - 12:34 -- Open Access
Author(s): 
Zuchelkowski BE, Wang L, Gingras S, Xu Q, Yang M, Triulzi D, Page GP, Gordeuk VR, Kim-Shapiro DB, Lee JS, Gladwin MT
Reference: 
PLoS One. 2020 Oct 2;15(10):e0240266

Hydroxychloroquine (HCQ) is widely used in the treatment of malaria, rheumatologic disease such as lupus, and most recently, COVID-19. These uses raise concerns about its safe use in the setting of glucose-6-phosphate dehydrogenase (G6PD) deficiency, especially as 11% of African American men carry the G6PD A- variant. However, limited data exist regarding the safety of HCQ in this population.

Interaction of Hydroxychloroquine with Pharmacokinetically Important Drug Transporters

October 1, 2020 - 15:20 -- Open Access
Author(s): 
Weiss J, Bajraktari-Sylejmani G, Haefeli WE
Reference: 
Pharmaceutics. 2020 Sep 25;12(10):E919

Hydroxychloroquine is used to treat malaria and autoimmune diseases, and its potential use against COVID-19 is currently under investigation. Thus far, information on interactions of hydroxychloroquine with drug transporters mediating drug-drug interactions is limited. We assessed the inhibition of important efflux (P-glycoprotein (P-gp), breast cancer resistance protein (BCRP)) and uptake transporters (organic anion transporting polypeptide (OATP)-1B1, OATP1B3, OATP2B1) by hydroxychloroquine, tested its P-gp and BCRP substrate characteristics, and evaluated the induction of pharmacokinetically relevant genes regulated by the nuclear pregnane X (PXR) (CYP3A4, ABCB1) and aryl hydrocarbon receptor (AhR) (CYP1A1, CYP1A2).

Chloroquine against malaria, cancers and viral diseases

September 23, 2020 - 08:44 -- Open Access
Author(s): 
Zhou W, Wang H, Yang Y, Chen ZS, Zou C, Zhang J
Reference: 
Drug Discov Today. 2020 Sep 16:S1359-6446(20)30367-6

Quinoline (QN) derivatives are often used for the prophylaxis and treatment of malaria. Chloroquine (CQ), a protonated, weakly basic drug, exerts its antimalarial effect mainly by increasing pH and accumulating in the food vacuole of the parasites.

Chloroquine and Hydroxychloroquine in the Treatment of Malaria and Repurposing in Treating COVID-19

September 15, 2020 - 14:44 -- Open Access
Author(s): 
Lei ZN, Wu ZX, Dong S, Yang DH, Zhang L, Ke Z, Zou C, Chen ZS
Reference: 
Pharmacol Ther. 2020 Sep 7:107672

Chloroquine (CQ) and Hydroxychloroquine (HCQ) have been commonly used for the treatment and prevention of malaria, and the treatment of autoimmune diseases for several decades. As their new mechanisms of actions are identified in recent years, CQ and HCQ have wider therapeutic applications, one of which is to treat viral infectious diseases.

Suspected Hydroxychloroquine-Induced Sinus Bradycardia and QTc Prolongation in a Patient with COVID-19

September 15, 2020 - 14:37 -- Open Access
Author(s): 
Kang Y, Wang H, Chen H, Wang B, Yang Y, Zhao X, Ran Q, Wei J
Reference: 
Int Heart J. 2020 Sep 12

An 84-year-old woman with hypertension, Alzheimer's disease, and chronic kidney disease presented with fever and was diagnosed with corona virus disease 2019 (COVID-19).

Hydroxychloroquine and Chloroquine Prescribing Patterns by Provider Specialty Following Initial Reports of Potential Benefit for COVID-19 Treatment - United States, January-June 2020

September 8, 2020 - 11:39 -- Open Access
Author(s): 
Bull-Otterson L, Gray EB, Budnitz DS, Strosnider HM, Schieber LZ, Courtney J, García MC, Brooks JT, Mac Kenzie WR, Gundlapalli AV
Reference: 
MMWR Morb Mortal Wkly Rep. 2020 Sep 4;69(35):1210-1215

Hydroxychloroquine and chloroquine, primarily used to treat autoimmune diseases and to prevent and treat malaria, received national attention in early March 2020, as potential treatment and prophylaxis for coronavirus disease 2019 (COVID-19) (1). On March 20, the Food and Drug Administration (FDA) issued an emergency use authorization (EUA) for chloroquine phosphate and hydroxychloroquine sulfate in the Strategic National Stockpile to be used by licensed health care providers to treat patients hospitalized with COVID-19 when the providers determine the potential benefit outweighs the potential risk to the patient.

Impact of Hydroxychloroquine/Chloroquine in COVID-19 Therapy: Two Sides of the Coin

September 8, 2020 - 11:36 -- Open Access
Author(s): 
Fatima U, Rizvi SSA, Fatima S, Hassan MI
Reference: 
J Interferon Cytokine Res. 2020 Sep 1

Coronavirus disease 2019 (COVID-19), which is caused by a novel severe acute respiratory syndrome coronavirus (SARS-CoV-2), has recently emerged as a global health threat. To address this health emergency, various therapeutic approaches are currently under investigation. There is limited evidence on the effectiveness of hydroxychloroquine (HCQ) and chloroquine (CQ) as COVID-19 therapies, and thus World Health Organization (WHO) mentioned that "Current data shows that this drug does not reduce deaths among hospitalized COVID-19 patients, nor help people with mild or moderate disease."

Antitussive noscapine and antiviral drug conjugates as arsenal against COVID-19: a comprehensive chemoinformatics analysis

August 24, 2020 - 13:13 -- Open Access
Author(s): 
Kumar N, Awasthi A, Kumari A, Sood D, Jain P, Singh T, Sharma N, Grover A, Chandra R
Reference: 
J Biomol Struct Dyn. 2020 Aug 20:1-16

Coronavirus pandemic has caused a vast number of deaths worldwide. Thus creating an urgent need to develop effective counteragents against novel coronavirus disease (COVID-19). Many antiviral drugs have been repurposed for treatment but implicated minimal recovery, which further advanced the need for clearer insights and innovation to derive effective therapeutics. Strategically, Noscapine, an approved antitussive drug with positive effects on lung linings may show favorable outcomes synergistically with antiviral drugs in trials.

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