TW201408304A - A combined drug with anti-cancer drug and hormone to treat renal cell carcinoma and its method of fabrication - Google Patents
A combined drug with anti-cancer drug and hormone to treat renal cell carcinoma and its method of fabrication Download PDFInfo
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- TW201408304A TW201408304A TW101131644A TW101131644A TW201408304A TW 201408304 A TW201408304 A TW 201408304A TW 101131644 A TW101131644 A TW 101131644A TW 101131644 A TW101131644 A TW 101131644A TW 201408304 A TW201408304 A TW 201408304A
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- cancer
- drug
- estrogen
- renal cell
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- 208000006265 Renal cell carcinoma Diseases 0.000 title claims abstract description 13
- 229940079593 drug Drugs 0.000 title claims description 7
- 239000003814 drug Substances 0.000 title claims description 7
- 238000004519 manufacturing process Methods 0.000 title claims 2
- 239000002246 antineoplastic agent Substances 0.000 title abstract description 11
- 229940041181 antineoplastic drug Drugs 0.000 title abstract description 6
- 229940088597 hormone Drugs 0.000 title description 2
- 239000005556 hormone Substances 0.000 title description 2
- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 claims abstract description 10
- 229930012538 Paclitaxel Natural products 0.000 claims abstract description 7
- 229960001592 paclitaxel Drugs 0.000 claims abstract description 7
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims abstract description 7
- 229960005309 estradiol Drugs 0.000 claims abstract description 6
- 239000003560 cancer drug Substances 0.000 claims description 3
- 229930182833 estradiol Natural products 0.000 claims description 3
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims description 3
- 238000002156 mixing Methods 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 abstract description 8
- 201000011510 cancer Diseases 0.000 abstract description 7
- 230000006907 apoptotic process Effects 0.000 abstract description 4
- 229940011871 estrogen Drugs 0.000 abstract description 4
- 239000000262 estrogen Substances 0.000 abstract description 4
- 108010038795 estrogen receptors Proteins 0.000 abstract description 3
- 239000003163 gonadal steroid hormone Substances 0.000 abstract description 3
- 230000036542 oxidative stress Effects 0.000 abstract description 3
- 229940127089 cytotoxic agent Drugs 0.000 abstract 2
- 102000015694 estrogen receptors Human genes 0.000 abstract 2
- 208000008839 Kidney Neoplasms Diseases 0.000 abstract 1
- 206010038389 Renal cancer Diseases 0.000 abstract 1
- 238000010609 cell counting kit-8 assay Methods 0.000 abstract 1
- 230000004663 cell proliferation Effects 0.000 abstract 1
- 230000003054 hormonal effect Effects 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 230000003834 intracellular effect Effects 0.000 abstract 1
- 201000010982 kidney cancer Diseases 0.000 abstract 1
- 230000001681 protective effect Effects 0.000 abstract 1
- 239000003642 reactive oxygen metabolite Substances 0.000 abstract 1
- 230000002195 synergetic effect Effects 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
- 210000004027 cell Anatomy 0.000 description 7
- 230000000694 effects Effects 0.000 description 7
- MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 description 4
- 102100038595 Estrogen receptor Human genes 0.000 description 3
- 229940044683 chemotherapy drug Drugs 0.000 description 3
- 206010019280 Heart failures Diseases 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 2
- 239000002147 L01XE04 - Sunitinib Substances 0.000 description 2
- 230000001093 anti-cancer Effects 0.000 description 2
- 239000013642 negative control Substances 0.000 description 2
- 239000013641 positive control Substances 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- 229960001796 sunitinib Drugs 0.000 description 2
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 description 2
- 201000009030 Carcinoma Diseases 0.000 description 1
- 206010059866 Drug resistance Diseases 0.000 description 1
- 108010007005 Estrogen Receptor alpha Proteins 0.000 description 1
- 101000882584 Homo sapiens Estrogen receptor Proteins 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 238000010586 diagram Methods 0.000 description 1
- 210000003292 kidney cell Anatomy 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 238000004064 recycling Methods 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
本發明是首次發展出結合抗癌藥物〈paclitaxel〉與性荷爾蒙〈17β-estradiol〉之抗腎細胞癌藥物。 The present invention is the first to develop an anti-renal cell cancer drug combining the anticancer drug <paclitaxel> and the sex hormone <17β-estradiol>.
先前技術腎細胞癌臨床標靶藥物Sunitinib,會造成嚴重副作用,諸如心臟衰竭、高血壓等;且價格昂貴,病患使用越久,負擔越大;況且經過長時間使用後,還是會有抗藥性的問題而失效;換言之,使用該藥物付出的代價與可回收的效益不成正比。 The prior art renal cell carcinoma clinical target drug Sunitinib, which causes serious side effects such as heart failure, high blood pressure, etc.; and is expensive, the longer the patient is used, the greater the burden; and after a long period of use, there is still resistance. The problem fails; in other words, the cost of using the drug is not proportional to the benefit of recycling.
先前技術腎細胞癌臨床標靶藥物Sunitinib會造成嚴重副作用,諸如心臟衰竭、高血壓等;且價格昂貴,病患使用越久,負擔越大;況且經過長時間使用後,還是會有抗藥性的問題而失效;換言之,使用該藥物付出的代價與可回收的效益不成正比。 Prior clinical kidney cell cancer clinical target drug Sunitinib can cause serious side effects, such as heart failure, high blood pressure, etc.; and expensive, the longer the patient uses, the greater the burden; and after a long period of use, there will still be resistance problems And fail; in other words, the cost of using the drug is not proportional to the benefit of recyclability.
1.利用雌激素〈如17β-estradiol〉可自由通透細胞膜。進入細胞後,其結合並激活雌激素受體〈estrogen receptor 1,ESR1〉,接著引發許多基因的表現之特性,以加乘抗癌藥物的效果,致使癌細胞發生細胞凋亡,促進癌細胞相對生長率顯著下降。 1. Use estrogen such as 17β-estradiol to freely penetrate the cell membrane. After entering the cell, it binds to and activates the estrogen receptor <estrogen receptor 1, ESR1>, and then triggers the characteristics of many genes to multiply the effect of anticancer drugs, causing cancer cells to undergo apoptosis and promoting cancer cell relative The growth rate is significantly reduced.
2.如「第一圖」所示,合併使用雌激素與太平洋紫杉醇者,腎細胞癌相對生長率下降至41.8%,相較於單純使用太平洋紫杉醇之對造組(細胞癌相對生長率49.9%),確實有加乘抗癌藥物的效果。 2. As shown in the "Picture 1", the relative growth rate of renal cell carcinoma decreased to 41.8% in combination with estrogen and paclitaxel, compared with the use of paclitaxel alone (the relative growth rate of cell carcinoma was 49.9%). ), there is indeed the effect of adding anti-cancer drugs.
2.如「第二圖」所示,藍色標示部分乃陰性對照組(控制組),而綠色部分為添加雙氧水後之陽性對照組;而紅色部分則為本發明(化療藥物合併性荷爾蒙),該組曲線由陰性對照組向添加雙氧水之陽性對照組移動,證明本發明能夠促進細胞產生氧化壓力,從而促使癌細胞因氧化而凋亡。 2. As shown in the "second figure", the blue part is the negative control group (control group), and the green part is the positive control group after adding hydrogen peroxide; the red part is the invention (chemotherapeutic drug combined hormone) The curve of this group was moved from the negative control group to the positive control group supplemented with hydrogen peroxide, which proved that the present invention can promote the oxidative stress of the cells, thereby promoting the apoptosis of the cancer cells due to oxidation.
1.本發明在相同濃度或劑量化療藥物之下,能達到更好的抗癌效果。 1. The present invention can achieve better anticancer effects under the same concentration or dose of chemotherapeutic drugs.
2.本發明在相同的抗癌效果之下,能夠減輕化療藥物之使用量,從而達到減少副作用、減輕藥物費用、降低抗藥性等之功效。 2. The invention can reduce the amount of chemotherapeutic drugs under the same anti-cancer effect, thereby achieving the effects of reducing side effects, reducing drug costs, and reducing drug resistance.
混和雌二醇與太平洋紫杉醇,以成為新抗腎細胞癌藥物。 Estradiol and paclitaxel are mixed to become a new anti-renal cell cancer drug.
第一圖:「本發明加乘抗癌藥物效果」示意圖。 First picture: Schematic diagram of "the effect of adding the anticancer drug of the present invention".
第二圖:「本發明促進細胞產生氧化壓力」示意圖。 Second figure: "The present invention promotes the generation of oxidative stress in cells".
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TW101131644A TW201408304A (en) | 2012-08-31 | 2012-08-31 | A combined drug with anti-cancer drug and hormone to treat renal cell carcinoma and its method of fabrication |
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Cited By (6)
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WO2019231498A1 (en) * | 2018-05-31 | 2019-12-05 | Crititech, Inc. | Treatment of kidney tumors by intratumoral injection of taxane particles |
US10507181B2 (en) | 2017-06-14 | 2019-12-17 | Crititech, Inc. | Methods for treating lung disorders |
US10507195B2 (en) | 2015-06-04 | 2019-12-17 | Crititech, Inc. | Taxane particles and their use |
US10874660B2 (en) | 2016-04-04 | 2020-12-29 | CritlTech, Inc. | Methods for solid tumor treatment |
US11058639B2 (en) | 2017-10-03 | 2021-07-13 | Crititech, Inc. | Local delivery of antineoplastic particles in combination with systemic delivery of immunotherapeutic agents for the treatment of cancer |
US11523983B2 (en) | 2017-06-09 | 2022-12-13 | Crititech, Inc. | Treatment of epithelial cysts by intracystic injection of antineoplastic particles |
-
2012
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US10507195B2 (en) | 2015-06-04 | 2019-12-17 | Crititech, Inc. | Taxane particles and their use |
US10729673B2 (en) | 2015-06-04 | 2020-08-04 | Crititech, Inc. | Taxane particles and their use |
US10993927B2 (en) | 2015-06-04 | 2021-05-04 | Crititech, Inc. | Taxane particles and their use |
US11458133B2 (en) | 2016-04-04 | 2022-10-04 | Crititech, Inc. | Methods for solid tumor treatment |
US10874660B2 (en) | 2016-04-04 | 2020-12-29 | CritlTech, Inc. | Methods for solid tumor treatment |
US10894045B2 (en) | 2016-04-04 | 2021-01-19 | Crititech, Inc. | Methods for solid tumor treatment |
US11033542B2 (en) | 2016-04-04 | 2021-06-15 | Crititech, Inc. | Methods for solid tumor treatment |
US11523983B2 (en) | 2017-06-09 | 2022-12-13 | Crititech, Inc. | Treatment of epithelial cysts by intracystic injection of antineoplastic particles |
US11737972B2 (en) | 2017-06-09 | 2023-08-29 | Crititech, Inc. | Treatment of epithelial cysts by intracystic injection of antineoplastic particles |
US12128131B2 (en) | 2017-06-09 | 2024-10-29 | Crititech, Inc. | Treatment of epithelial cysts by intracystic injection of antineoplastic particles |
US11160754B2 (en) | 2017-06-14 | 2021-11-02 | Crititech, Inc. | Methods for treating lung disorders |
US10507181B2 (en) | 2017-06-14 | 2019-12-17 | Crititech, Inc. | Methods for treating lung disorders |
US11058639B2 (en) | 2017-10-03 | 2021-07-13 | Crititech, Inc. | Local delivery of antineoplastic particles in combination with systemic delivery of immunotherapeutic agents for the treatment of cancer |
US11583499B2 (en) | 2017-10-03 | 2023-02-21 | Crititech, Inc. | Local delivery of antineoplastic particles in combination with systemic delivery of immunotherapeutic agents for the treatment of cancer |
US11918691B2 (en) | 2017-10-03 | 2024-03-05 | Crititech, Inc. | Local delivery of antineoplastic particles in combination with systemic delivery of immunotherapeutic agents for the treatment of cancer |
US12329858B2 (en) | 2017-10-03 | 2025-06-17 | Crititech, Inc. | Local delivery of antineoplastic particles in combination with systemic delivery of immunotherapeutic agents for the treatment of cancer |
WO2019231498A1 (en) * | 2018-05-31 | 2019-12-05 | Crititech, Inc. | Treatment of kidney tumors by intratumoral injection of taxane particles |
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