Interactions of azole antifungal agents with the human breast cancer resistance protein (BCRP)

Gupta, Anshul; Unadkat, Jashvant D.; Mao, Qingcheng

doi:10.1002/jps.20963

Cited by 78 publications

(58 citation statements)

References 34 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…170 Inhibitor of BCRP. 163 No inhibition of NTCP or BSEP. 170 CYP3A4 inhibition will affect metabolism of a variety of drugs to increase their levels (e.g., BU, 171 dexamethasone, 172 midazolam, 173 ciclosporin, 174 tacrolimus, 174 methyl-prednisolone 175 ) or the levels of their metabolites.…”

Section: Interaction Commentsmentioning

confidence: 99%

“…160 No inhibition of P-gp [160][161][162] or BCRP. 163 Interaction with ciclosporin via CYP inhibition causes increased ciclosporin levels, especially with oral fluconazole. 164,165 Itraconazole Substrate for CYP3A4; 57 potent inhibitor of CYP3A4 160 and less so for CYP2C9, CYP2C19.…”

Section: Interaction Commentsmentioning

confidence: 99%

“…179 No inhibition of BCRP. 163 CYP interaction probably accounts for the interaction of voriconazole with many drugs, causing increased levels of tacrolimus, 180 ciclosporin, 181 increased VCR neurotoxicity 182 and reduced clearance of midazolam, 183 particularly the oral formulation of midazolam. Concomitant use of rifabutin, 184 an inducer of CYP and especially of CYP3A4, causes significant reduction in voriconazole levels.…”

Section: Interaction Commentsmentioning

confidence: 99%

See 2 more Smart Citations

Has the era of individualised medicine arrived for antifungals? A review of antifungal pharmacogenomics

Ashbee

Gilleece

2011

Bone Marrow Transplant

View full text Add to dashboard Cite

Section: Interaction Commentsmentioning

confidence: 99%

Section: Interaction Commentsmentioning

confidence: 99%

Section: Interaction Commentsmentioning

confidence: 99%

See 1 more Smart Citation

Has the era of individualised medicine arrived for antifungals? A review of antifungal pharmacogenomics

Ashbee

Gilleece

2011

Bone Marrow Transplant

View full text Add to dashboard Cite

“…1; Table I) (4)(5)(6). In addition, the human breast cancer resistance protein is also inhibited by itraconazole (7).…”

Section: Preclinical Datamentioning

confidence: 99%

Repurposing itraconazole as an anticancer agent

et al. 2017

View full text Add to dashboard Cite

Abstract. Itraconazole, a common anti-fungal agent, has demonstrated potential anticancer activity, including reversing chemoresistance mediated by P-glycoprotein, modulating the signal transduction pathways of Hedgehog, mechanistic target of rapamycin and Wnt/β-catenin in cancer cells, inhibiting angiogenesis and lymphangiogenesis, and possibly interfering with cancer-stromal cell interactions. Clinical trials have suggested the clinical benefits of itraconazole monotherapy for prostate cancer and basal cell carcinoma, as well as the survival advantage of combination chemotherapy for relapsed non-small cell lung, ovarian, triple negative breast, pancreatic and biliary tract cancer. As drug repurposing is cost-effective and timesaving, a review was conducted of preclinical and clinical data focusing on the anticancer activity of itraconazole, and discusses the future directions for repurposing itraconazole as an anticancer agent.

show abstract

“…In vitro studies confirm that itraconazole inhibits the efflux pump, thus reversing resistance (10,14,19,20). This has also been observed in resistant leukaemia and human embryonic kidney cells (21,22). …”

Section: Itraconazole and Drug Resistancementioning

confidence: 61%

Repurposing itraconazole for the treatment of cancer

et al. 2017

View full text Add to dashboard Cite

Abstract. The repurposing of drugs is becoming increasingly attractive as it avoids the lengthy process and cost implications associated with bringing a novel drug to market. Itraconazole is a broad-spectrum anti-fungal agent. An emerging body of in vivo, in vitro and clinical evidence have confirmed that it also possesses antineoplastic activities and has a synergistic action when combined with other chemotherapeutic agents. It acts via several mechanisms to prevent tumour growth, including inhibition of the Hedgehog pathway, prevention of angiogenesis, decreased endothelial cell proliferation, cell cycle arrest and induction of auto-phagocytosis. These allow itraconazole, either alone or in combination with other cytotoxic agents, to increase drug efficacy and overcome drug resistance. This study reviews the reported literature on the use of itraconazole in a variety of malignancies and highlights the recent insights into the critical pathways acted upon to prevent tumour growth.

show abstract

Interactions of azole antifungal agents with the human breast cancer resistance protein (BCRP)

Cited by 78 publications

References 34 publications

Has the era of individualised medicine arrived for antifungals? A review of antifungal pharmacogenomics

Has the era of individualised medicine arrived for antifungals? A review of antifungal pharmacogenomics

Repurposing itraconazole as an anticancer agent

Repurposing itraconazole for the treatment of cancer

Contact Info

Product

Resources

About