6533b835fe1ef96bd12a0134
RESEARCH PRODUCT
Cancer combination therapy of the sesquiterpenoid artesunate and the selective EGFR-tyrosine kinase inhibitor erlotinib.
Thomas EfferthThomas A. Efferthsubject
0301 basic medicineCombination therapymedicine.medical_treatmentPharmaceutical ScienceArtesunateDrug resistancePharmacology03 medical and health scienceschemistry.chemical_compoundErlotinib Hydrochloride0302 clinical medicineIn vivoDrug DiscoveryAntineoplastic Combined Chemotherapy ProtocolsMedicineHumansEpidermal growth factor receptorMolecular Targeted TherapyProtein Kinase InhibitorsPharmacologyChemotherapybiologybusiness.industryCancermedicine.diseaseArtemisininsErbB Receptors030104 developmental biologyComplementary and alternative medicinechemistryArtesunate030220 oncology & carcinogenesisbiology.proteinMolecular MedicineErlotinibbusinessmedicine.drugdescription
Abstract Background The shift from cytotoxic to targeted chemotherapy led to improved treatment outcomes in oncology. Nevertheless, many cancer patients cannot be cured from their disease because of the development of drug resistance and side effects. Purpose There is an ongoing quest for novel compounds, which raised not only the interest in natural products but also in novel combination therapy regimens. Study design In this review, we report on the inhibition epidermal growth factor receptor (EGFR) by targeted small molecules and their combination with natural products from medicinal plants. Results The combination of erlotinib with artesunate leads to synergistic inhibition of cell growth in isobologram analyses. Artesunate is an approved anti-malaria drug, which is also active against cancer as shown in vitro, in vivo and in preliminary clinical phase I/II trials. Conclusion The combination of natural products (e.g. the sesquiterpenoid artesunate) and synthetic compounds (e.g. the small molecule EGFR tyrosine kinase inhibitor erlotinib) may lead to improved clinical success rates in oncology.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2017-12-01 | Phytomedicine : international journal of phytotherapy and phytopharmacology |