Novel combinations of a tubulin polymerization inhibitor and a poly (adp-ribose) polymerase (PARP) inhibitor for use in the treatment of cancer
A technology of polymerization inhibitor and tubulin, which can be used in medical preparations containing active ingredients, anti-tumor drugs, anti-infective drugs, etc., and can solve problems such as unmet medical needs.
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Embodiment 1
[0200] Antitumor Efficacy of NOV202 Alone and in Combination with Olaparib in Patient-Derived Ovarian Cancer Xenografts (Ov10584)
[0201] NMRI was used as follows: nu / nu female (Janvier) mice (8 weeks old): 4 animals in the vehicle group, 4 animals each in the NOV202 group, olaparib group, and the combination group of NOV202 and olaparib. only animals. NOV202 was synthesized as described in WO2012 / 127032. Olaparib was purchased from LC Laboratories. Patient-derived xenograft Ov10584 was used at passage number 7. On day 0, all mice received 2x2mm tissue fragments subcutaneously and tumors were allowed to reach 118mm before starting treatment 3 (average) palpable size (study day 8). The NOV202 group was administered PO at a dose of 30 mg / kg, and the olaparib group was administered PO at a dose of 100 mg / kg. The combination arm of NOV202 and olaparib has the same dose and schedule as monotherapy. NOV202 (5ml / kg) was administered in the morning and olaparib (10ml / kg) in the...
Embodiment 2
[0205] Antitumor Efficacy of NOV202 in Combination with Olaparib and Combination of Plinabulin and Olaparib in Patient-Derived Ovarian Cancer Xenografts (Ov10584)
[0206] NMRI was used as follows: nu / nu female (Janvier) mice (8 weeks old): 4 animals in the vehicle group, in the NOV202, olaparib, plinabulin, NOV202 and olaparib groups There were 4 animals in the combination group of Plinabulin and Olaparib respectively. NOV202 was synthesized as described in WO 2012 / 127032. Olaparib was purchased from LC Laboratories and Plinabulin was purchased from Sellechem. Patient-derived xenograft Ov10584 was used at passage number 4. On day 0, all mice received 2x2mm tissue fragments subcutaneously into the left flank, and tumors were allowed to reach 108mm before starting treatment 3 (average) palpable size (study day 6). The NOV202 group was administered PO at a dose of 30 mg / kg, and the olaparib group was administered PO at a dose of 100 mg / kg, and Plinabulin was administered int...
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