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    • 1. 发明申请
    • METHOD FOR ENHANCING PDT EFFICACY USING A TYROSINE KINASE INHIBITOR
    • 使用酪氨酸激酶抑制剂增强PDT效率的方法
    • WO2008008215A3
    • 2008-09-04
    • PCT/US2007015263
    • 2007-06-29
    • HEALTH RESEARCH INCPANDEY RAVINDRA KOSEROFF ALLANMORGAN JANETZHENG XIANGWEIGUO LIU
    • PANDEY RAVINDRA KOSEROFF ALLANMORGAN JANETZHENG XIANGWEIGUO LIU
    • A61K31/409
    • A61K31/409A61K41/0061A61K41/0071
    • A method for treating hyperproliferative tissue in a mammal which tissue expresses ABCG2 including the steps of: a) systemically introducing from about 100 to about 1000 mg/kg of body weight of a tyrosine kinase inhibiting compound into the mammal; b) within from about 0.5 to about 24 hours after the introducing in step a) systemically introducing from about 0.05 to about 0.5 µmol per kilogram of body weight of a tumor avid photosensitizing compound, that acts as a substrate for ABC family transport protein, ABCG2 and that has a preferential light absorbance frequency; and c) exposing the hyperproliferative tissue to light at a fluence of from about 50 to about 150 J/cm 2 delivered at a rate of from about 5 to about 25 mW/cm 2 at the light absorbance frequency. The photosensitizing compound is preferably a tetrapyrollic photosensitizer compound where the tetrapyrollic compound is a chlorin, bacteriochlorin, porphyrin, pheophorbide including pyropheophorbides, purpurinimide, or bacteriopurpurinimide and derivatives thereof; provided that, the photosensizing compound is not a meso-tetra (3-hydroxyphenyl) derivative, is not a saccharide derivative and is not a hematoporphyrin.
    • 一种用于治疗组织表达ABCG2的哺乳动物的过度增殖组织的方法,包括以下步骤:a)将约100至约1000mg / kg体重的酪氨酸激酶抑制化合物全身引入哺乳动物; b)在步骤a)中引入后约0.5至约24小时内,全身引入约0.05至约0.5μmol/千克体重的肿瘤avid光敏化合物,其作为ABC家族转运蛋白ABCG2的底物 并具有优先吸光度频率; 并且c)将过度增殖组织以约5至约25mW / cm 2的速率递送的约50至约150J / cm 2的能量密度曝光, SUP>在吸光度频率。 光敏化合物优选为四级光敏剂化合物,其中四味化合物是二氢卟酚,细菌二氢卟酚,卟啉,含有偏高双歧杆菌,嘌呤酰亚胺或嘌呤嘌呤酰亚胺及其衍生物的脱镁叶绿素; 光敏化合物不是内消旋 - 四(3-羟基苯基)衍生物,不是糖衍生物,不是血卟啉。
    • 2. 发明申请
    • METHOD FOR ENHANCING PDT EFFICACY USING A TYROSINE KINASE INHIBITOR
    • 利用酪氨酸激酶抑制剂增强PDT功效的方法
    • WO2008008215A2
    • 2008-01-17
    • PCT/US2007/015263
    • 2007-06-29
    • HEALTH RESEARCH, INC.PANDEY, Ravindra, K.OSEROFF, AllanMORGAN, JanetZHENG, XiangWEIGUO, Liu
    • PANDEY, Ravindra, K.OSEROFF, AllanMORGAN, JanetZHENG, XiangWEIGUO, Liu
    • A61K31/409
    • A61K31/409A61K41/0061A61K41/0071
    • A method for treating hyperproliferative tissue in a mammal which tissue expresses ABCG2 including the steps of: a) systemically introducing from about 100 to about 1000 mg/kg of body weight of a tyrosine kinase inhibiting compound into the mammal; b) within from about 0.5 to about 24 hours after the introducing in step a) systemically introducing from about 0.05 to about 0.5 μmol per kilogram of body weight of a tumor avid photosensitizing compound, that acts as a substrate for ABC family transport protein, ABCG2 and that has a preferential light absorbance frequency; and c) exposing the hyperproliferative tissue to light at a fluence of from about 50 to about 150 J/cm 2 delivered at a rate of from about 5 to about 25 mW/cm 2 at the light absorbance frequency. The photosensitizing compound is preferably a tetrapyrollic photosensitizer compound where the tetrapyrollic compound is a chlorin, bacteriochlorin, porphyrin, pheophorbide including pyropheophorbides, purpurinimide, or bacteriopurpurinimide and derivatives thereof; provided that, the photosensizing compound is not a meso-tetra (3-hydroxyphenyl) derivative, is not a saccharide derivative and is not a hematoporphyrin.
    • 一种治疗哺乳动物中过度增殖组织的方法,所述组织表达ABCG2,所述方法包括以下步骤:a)将约100至约1000mg / kg体重的酪氨酸激酶抑制性化合物全身性地引入 哺乳动物; b)在步骤a)中引入约0.5至约24小时后,系统地引入约0.05至约0.5μmol/千克体重的肿瘤亲合性光敏化合物,其充当ABC家族转运蛋白ABCG2的底物 并且具有优先的光吸收频率; 和c)以约5至约25mW / cm 2的速率递送约50至约150J / cm 2的能量密度将过度增殖组织暴露于光下, 在光吸收频率下。 光敏化合物优选四吡咯类光敏剂化合物,其中四吡咯化合物为二氢卟酚,菌绿素,卟啉,脱镁叶绿酸包括焦脱镁叶绿酸,紫红素酰亚胺或细菌嘌呤亚胺及其衍生物; 条件是,光敏化合物不是一种内消旋 - 四(3-羟基苯基)衍生物,不是糖衍生物,也不是血卟啉。