生物活性

• 描述Chloroquine diphosphate (CQ), an autophagy inhibitor that may enhance the cytocidal effect of gefitinib against cSCC, was used in the present study. Suppression of autophagy by CQ, which was demonstrated by an alteration in microtubule associated protein 1 light chain 3-B in CQ pre-treated A431 cells, significantly enhanced cell apoptosis, which suggested that gefitinib-induced autophagy is cytoprotective. CQ was demonstrated to exhibit a synergistic apoptotic effect when used in combination with gefitinib during cSCC(cutaneous squamous cell carcinoma) therapy^[2]. In vitro studies indicate that the antiviral effect of chloroquine diphosphate (CQ) requires a high concentration of the drug^[3]. Chloroquine diphosphate (25mg/kg and 50mg/kg, respectively) significantly inhibited the growth of the implanted 4T1 tumor cells and induced apoptosis in the tumor microenvironment. Moreover, the metastasis of tumor cells to the lungs was inhibited significantly and the survival of the mice enhanced^[4].
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  human HeLa cells	-	Cytotoxic assay	-	Cytotoxicity against human HeLa cells assessed as growth inhibition by MTT assay, IC50=30 μM	24354322
  human HepG2 cells	-	Cytotoxic assay	48 h	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay, IC50=37.68 μM	23815186
  human K562 cells	-	Cytotoxic assay	-	Cytotoxicity against human K562 cells by MTT assay, IC50=31.83 nM	18538567

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• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02563496	Malaria, Vivax	Phase 2	Recruiting	November 30, 2019	Colombia ... more >> GSK Investigational Site Recruiting Monteria, Colombia Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com    Thailand GSK Investigational Site Not yet recruiting Tak, Thailand, 63110 Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com    Vietnam GSK Investigational Site Recruiting Hanoi, Vietnam, 100000 Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com    GSK Investigational Site Recruiting Ho Chi Minh City, Vietnam, 700000 Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com    GSK Investigational Site Recruiting Ho Chi Minh, Vietnam Contact: US GSK Clinical Trials Call Center    877-379-3718    GSKClinicalSupportHD@gsk.com    Contact: EU GSK Clinical Trials Call Center    +44 (0) 20 8990 4466    GSKClinicalSupportHD@gsk.com Collapse <<
  NCT01136850	Malaria in Pregnancy ... more >> Sexually Transmitted Infections Anaemia Collapse <<	Phase 3	Completed	-	Papua New Guinea ... more >> Papua New Guinea Institute of Medical Research Madang, Madang Province, Papua New Guinea Collapse <<
  NCT00157859	Falciparum Malaria ... more >> Vivax Malaria Collapse <<	Not Applicable	Completed	-	Indonesia ... more >> SP9 & SP12 Public Health- Malaria control clinics Timika, Papua, Indonesia Collapse <<

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• 参考文献

• [2] Wang J, Wang C, Hu X, Yu C, Zhou L, Ding Z, Zhou M. Gefitinib-mediated apoptosis is enhanced via inhibition of autophagy by chloroquine diphosphate in cutaneous squamous cell carcinoma cells. Oncol Lett. 2019 Jul;18(1):368-374

  [3] Borba MGS, Val FFA, Sampaio VS, Alexandre MAA, Melo GC, Brito M, Mourão MPG, Brito-Sousa JD, Baía-da-Silva D, Guerra MVF, Hajjar LA, Pinto RC, Balieiro AAS, Pacheco AGF, Santos JDO Jr, Naveca FG, Xavier MS, Siqueira AM, Schwarzbold A, Croda J, Nogueira ML, Romero GAS, Bassat Q, Fontes CJ, Albuquerque BC, Daniel-Ribeiro CT, Monteiro WM, Lacerda MVG; CloroCovid-19 Team. Effect of High vs Low Doses of Chloroquine Diphosphate as Adjunctive Therapy for Patients Hospitalized With Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) Infection: A Randomized Clinical Trial. JAMA Netw Open. 2020 Apr 24;3(4):e208857

  [4] Jiang PD, Zhao YL, Deng XQ, Mao YQ, Shi W, Tang QQ, Li ZG, Zheng YZ, Yang SY, Wei YQ. Antitumor and antimetastatic activities of chloroquine diphosphate in a murine model of breast cancer. Biomed Pharmacother. 2010 Nov;64(9):609-14