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Hydroxychloroquine inhibits KCNH2. 28 / 29
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"Our results showed that while chloroquine acutely blocked hERG current (I hERG) with an IC 50 of 3.0 microM, hydroxychloroquine acutely blocked I hERG 8-fold less potently, with an IC 50 of 23.4 microM."
33674391
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"We found that Chloroquine inhibits hERG, Nav1.5, and Cav1.2 channels, whereas Hydroxychloroquine inhibits hERG and Cav1.2 channels."
33483756
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"Hydroxychloroquine attenuates hERG channel by promoting the membrane channel degradation: computational simulation and experimental evidence for QT-interval prolongation with hydroxychloroquine treatment."
37231805
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"HCQ is known to block Kv11.1 ( HERG ) and induce prolong QT , thus predisposing the patient to malignant arrhythmia such as torsade de points.70 , 71 However , studies have found that these arrhythmic toxicities are mostly encountered in chronic use with multiple concomitant QT prolonging agents , metabolic abnormalities , renal insufficiency , as well as medication overdose.72 , 73 Because the use of HCQ in COVID-19 has relatively short duration , the risk of developing significant arrhythmia is relatively low ."
32959951
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"Key Results: Chloroquine and hydroxychloroquine blocked hERG with IC50 of 1.47±0.07 µM and 3.78±0.17 µM respectively, indicating proarrhythmic risk at concentrations effective against SARS-CoV-2 in vitro and proposed in COVID-19 clinical trials."
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"For instance, among COVID-19 treatment drugs, chloroquine and hydroxychloroquine were demonstrated to block hERG potassium channels, whereas azithromycin and remdesivir did not [143] ."
35336980
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"Hydroxychloroquine is known to block Kv11.1 ( HERG ) and can cause drug-induced long-QT syndrome [ 5 ] ."
32333026
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"Hydroxychloroquine is known to block Kv11.1 ( HERG ) and can cause drug-induced long QT ."
32228309
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"HCQ is known to block Kv11.1 ( HERG ) and can cause drug-induced LQT ."
32247013
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"Additionally, hERG channel inhibition by HCQ is stronger at lower extracellular K+ concentrations, [33] pointing to the need to correct or prevent hypokalaemia during and immediately after clinical therapy with this drug.The direct correlation between the QTc interval and age seen in our data has already been described in the literature [35]."
35553396
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"HCQ is not only known to mildly block the human ether-a-go-go related gene (hERG) aka KCNH2 that codes for delayed rectifier potassium channel, but also the inward-rectifier potassium channel [XREF_BIBR]."
33386447
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"[35]However, hydroxychloroquine is a known inhibitor of the KCNH2-encoded hERG/Kv11.1 potassium channel present in the heart."
34584623
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"The combination of HCQ, FQs, and remdesivir may synergistically inhibit hERG channels, and disrupt repolarization reserve, since remdesivir was also reported to block K + currents ( Chang, Liu et al. [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
34058295
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"Chloroquine and hydroxychloroquine blocked hERG with IC 50 of 1.47±0.07 μM and 3.78±0.17 μM respectively, indicating proarrhythmic risk at concentrations effective against SARS-CoV-2 in vitro."
34837219
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"We previously hypothesized that the combination of azithromycin and chloroquine or hydroxychloroquine would be more likely to precipitate cardiac dysrhythmias than either alone because chloroquine and hydroxychloroquine also inhibit hERG [59]."
36525217
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"HCQ can block the KCNH2 encoded hERG and Kv11.1 potassium channel and thereby carries a risk of drug induced QT prolongation and cardiac arrest."
32835316
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"HCQ inhibits hERG (IKr) potassium channels, it is known to increase in QT interval of cardiomyocytes, and can induce arrhythmias that are responsible for sudden death [20]."
| DOI
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"KEY RESULTS Chloroquine and hydroxychloroquine blocked hERG with IC50 of 1.47 + / -0.07 muM and 3.78 + / -0.17 muM respectively , indicating proarrhythmic risk at concentrations effective against SARS-CoV-2 in vitro ."
34837219
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"Our results showed that while chloroquine acutely blocked hERG current (I hERG) with an IC 50 of 3.0 microM, hydroxychloroquine acutely blocked I hERG 8-fold less potently, with an IC50 of 23.4 microM."
| PMC
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"Finally, hydroxychloroquine blocks the KCNH2 encoded hERG and Kv11.1 potassium channel and can potentially prolong the corrected QT interval, with potentially severe consequences, such as sudden cardiac death and cardiac arrhythmia in patients with covid-19."
32409486
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"We found that the enantiomers of HCQ selectively inhibit K 2.1 channels and, less potently, hERG channels, and significantly alter several cardinal AP metrics at concentrations about one order of magnitude above the free plasma concentrations circulating at therapeutically effective doses.2 Material and methods."
34863995
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"The main mechanism of HCQ induced QT prolongation is blockage of hERG K + channels [XREF_BIBR]."
33095083
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"Additionally, for hydroxychloroquine, a recent study pointed out that hydroxychloroquine could lead to unwanted QT interval prolongation by blocking the KCNH2 encoded hERG and Kv11.1 potassium channel, thereby increasing the risk of drug induced torsade de pointes and sudden cardiac death."
32426374
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"Hydroxychloroquine is believed to act on the entry and post-entry stages of COVID-19 and blocks the hERG potassium channel, therefore potentially prolonging QTc [XREF_BIBR]."
33307378
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"Recently, a study of the effects of COVID-19 drugs chloroquine and hydroxychloroquine on blocking the hERG potassium channel showed that these drugs acutely and severely inhibited the hERG current, but remdesivir increased the I with promoted hERG maturation when acting alone (Szendrey et al., 2021)."
35873575
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"HCQ reduced the mature hERG protein in a time and concentration-dependent manner."
37231805
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"Treatment of Brefeldin A (BFA) and HCQ combination reduced hERG protein to a greater extent than BFA alone."
37231805
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"XREF_FIG shows that Hydroxychloroquine and Chloroquine inhibited the hERG current with IC50 values of 9.7 and 7.77 microM, respectively, but Azithromycin had no effect."
33483756