Differential effects of ketoconazole and primaquine on the pharmacokinetics and tissue distribution of imatinib in mice

Soo, Gian Wan; Law, Jason H K; Kan, Elaine; Tan, Shin Yee; Lim, Wei Yin; Chay, Grace; Bukhari, Nadeem Irfan; Segarra, Ignacio

doi:10.1097/cad.0b013e32833c93b3

Cited by 24 publications

(24 citation statements)

References 39 publications

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“…The brain penetration of imatinib is of special interest. In‐vitro studies have shown that glioma and glioblastoma cell lines are sensitive to imatinib [12,13] but animal studies do not show the expected activity, [14] probably because of limited brain penetration [15] caused by P‐gp and Bcrp1 efflux transporters present in the BBB [11] . However, concurrent administration with P‐gp substrates or inhibitors produces enhanced brain delivery [15] …”

Section: Discussionmentioning

confidence: 99%

“…Imatinib is the drug of choice for GIST treatment as a neoadjuvant prior to surgery and thereafter as adjuvant therapy [2] . Due to imatinib being a CYP3A4 and P‐gp substrate, potential interactions with drugs used during postoperative infections or their prophylaxis may take place, [1] causing pharmacokinetic and pharmacodynamic interactions [15] …”

Section: Introductionmentioning

confidence: 99%

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Metronidazole leads to enhanced uptake of imatinib in brain, liver and kidney without affecting its plasma pharmacokinetics in mice

Tan

Kan

Lim

et al. 2011

Journal of Pharmacy and Pharmacology

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Metronidazole leads to enhanced uptake of imatinib in brain, liver and kidney without affecting its plasma pharmacokinetics in mice

Tan

Kan

Lim

et al. 2011

Journal of Pharmacy and Pharmacology

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“…A number of studies have shown a relationship between cancer and malaria in regard to diagnostics, drug research, treatment, prevention, and epidemiology . Different classes of antimalarial drugs display direct or adjuvant activity against cancer cell lines, are known as sensitivity reversers of resistant tumor cell lines or inhibitors of drug resistance development, or have synergistic action with known anticancer drugs . Although their exact mode of action against cancer is still not completely understood, various mechanisms have been proposed …”

Section: Introductionmentioning

confidence: 99%

SAHAquines, Novel Hybrids Based on SAHA and Primaquine Motifs, as Potential Cytostatic and Antiplasmodial Agents

et al. 2018

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We report the synthesis of SAHAquines and related primaquine (PQ) derivatives. SAHAquines are novel hybrid compounds that combine moieties of suberoylanilide hydroxamic acid (SAHA), an anticancer agent with weak antiplasmodial activity, and PQ, an antimalarial drug with low antiproliferative activity. The preparation of SAHAquines is simple, cheap, and high yielding. It includes the following steps: coupling reaction between primaquine and a dicarboxylic acid monoester, hydrolysis, a new coupling reaction with O‐protected hydroxylamine, and deprotection. SAHAquines 5 a–d showed significant reduction in cell viability. Among the three human cancer cell lines (U2OS, HepG2, and MCF‐7), the most responsive were the MCF‐7 cells. The antibodies against acetylated histone H3K9/H3K14 in MCF‐7 cells revealed a significant enhancement following treatment with N‐hydroxy‐N′‐{4‐[(6‐methoxyquinolin‐8‐yl)amino]pentyl}pentanediamide (5 b). Ethyl (2E)‐3‐({4‐[(6‐methoxyquinolin‐8‐yl)amino]pentyl}carbamoyl)prop‐2‐enoate (2 b) and SAHAquines were the most active compounds against both the hepatic and erythrocytic stages of Plasmodium parasites, some of them at sub‐micromolar concentrations. The results of our research suggest that SAHAquines are promising leads for new anticancer and antimalarial agents.

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“…On the other hand, Soo et al reported that primaquine increases imatinib clearance, bioavailability, and distribution pattern, which could improve the treatment of chronic myelogenous leukemia [38]. Therefore, we still need more research to verify its effect in CLL.…”

Section: Discussionmentioning

confidence: 99%

Personalized Drug Analysis in B Cell Chronic Lymphocytic Leukemia Patients

Liu

Gao

et al. 2017

Med Sci Monit

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BackgroundB cell chronic lymphocytic leukemia (B-CLL) is the most common adult leukemia in the Western world. Although therapeutic advances have notably improved the outcome for many patients, B-CLL remains an incurable disease. The purpose of this study was to search for therapeutic drugs based on altered pathways in individual patients.Material/MethodsGenes from microarray data were mapped to 300 Homo sapiens-related pathways. Individual pathway aberrance analysis was used to identify altered pathways. Drug data, obtained from connectivity map (cMAP), were subjected to drug-set enrichment analysis. To analyze the relations between drug-induced pathways and disease-induced altered pathways in individuals, Pearson correlation analysis was applied.ResultsThe disease-induced pathways with P-values <0.05 in individual samples were recorded and presented in a heatmap. Drug-induced pathways were analyzed in the 104 samples. After Pearson correlation analysis between altered pathways and drug, the 20 top-ranked drugs that were most relevant to disease were obtained. There were 9 drugs with positive scores and 11 with negative scores.ConclusionsWith this method, we identified the 20 top-ranked drugs that were most relevant to disease. The drugs with negative scores may play therapeutic roles in B-CLL.

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Differential effects of ketoconazole and primaquine on the pharmacokinetics and tissue distribution of imatinib in mice

Cited by 24 publications

References 39 publications

Metronidazole leads to enhanced uptake of imatinib in brain, liver and kidney without affecting its plasma pharmacokinetics in mice

Metronidazole leads to enhanced uptake of imatinib in brain, liver and kidney without affecting its plasma pharmacokinetics in mice

SAHAquines, Novel Hybrids Based on SAHA and Primaquine Motifs, as Potential Cytostatic and Antiplasmodial Agents

Personalized Drug Analysis in B Cell Chronic Lymphocytic Leukemia Patients

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