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. 2022 Aug 16;13:959902. doi: 10.3389/fendo.2022.959902

Table 2.

Drugs which can increase the cholesterol and their potential to activate PXR.

Drug class Drug Mechanism The influence on cholesterol The influence on PXR Reference
Antibiotic Rifampicin Bacterial RNA synthesis inhibition CHOL&LDL↑ PXR agonist (135, 136)
Anticonvulsant Carbamazepine Blocking of central Na+ channel CHOL&LDL↑ PXR agonist (18, 137)
Antihypertensive Lacidipine Ca2+ channel blocker LDL↑ PXR agonist (138)
Antineoplastic Apalutamide Antiandrogen CHOL&LDL↑ Possible PXR agonist (139)
Mitotane Adrenal cortex inhibition CHOL&LDL↑ PXR agonist (140142)
Ruxolitinib JAK inhibition CHOL↑ Possible PXR agonist (98)
Brigatinib Tyrosine kinase inhibition CHOL&LDL↑ Possible PXR agonist (98)
Dasatinib Tyrosine kinase inhibition CHOL&LDL↑ PXR agonist (138)
Nilotinib Tyrosine kinase inhibition CHOL&LDL↑ PXR agonist (143)
Antipsychotic, atypical Quetiapine Inhibition of D2 and 5-HT2A receptors CHOL&LDL↑ PXR agonist (95)
Antiretroviral Efavirenz Non-nucleoside reverse transcriptase inhibition CHOL&LDL↑ PXR agonist (21, 144, 145)
Etravirine Non-nucleoside reverse transcriptase inhibition CHOL&LDL↑ PXR agonist (146149)
Rilpivirine Non-nucleoside reverse transcriptase inhibition CHOL&LDL↑ PXR agonist (146)
Darunavir Protease inhibition CHOL↑ PXR agonist (21)
Fosamprenavir Protease inhibition CHOL↑ PXR agonist (150)
Lopinavir Protease inhibition CHOL↑ PXR agonist (21)
Ritonavir Protease inhibition CHOL↑ PXR agonist (151)
Saquinavir Protease inhibition CHOL&LDL↑ PXR agonist (151)
Barbiturate Phenobarbital GABA stimulation LDL↑ PXR agonist (152, 153)
Immunosuppressant Cyclosporin Calcineurin inhibition CHOL&LDL↑ PXR agonist (154)
Tacrolimus Calcineurin inhibition CHOL↑ PXR agonist (155)
Dexamethasone Glucocorticoid receptor activation CHOL↑ PXR agonist (10, 156, 157)
Proton pump inhibitor Lansoprazole Stomach acid reduction CHOL↑ PXR agonist (158)
Stimulant Modafinil Dopaminergic modulation CHOL↑ PXR agonist (159)