藥學共筆
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分類: 2017studytogether、​2017、​抗癌藥、​
以及 其他5個分類

New Taiwanese Antineoplastics classification

編輯

Molecularly Targeted therapeutic agents靶向治療藥品:~mab[]

main article: ~mab

unconjugated monoclonal antibody:腫瘤特異性抗體（tumor-specific antibody）[]

0

單株抗體偶聯物（Antibody conjugates）[]

抗體藥物複合體/單株抗體藥品偶聯物（Antibody-drug conjugates）:由抗體導向的化學療法藥品 單株抗體結合毒殺藥物（antibody-drug conjugates, ADCs）[]

0

放射免疫治療（radioimmunotherapy）=單株抗體放射性同位素偶聯物（antibody-radionuclide conjugates, ARCs）[]

0

Molecularly Targeted therapeutic agents靶向治療藥品:Synthetic small molecule in targeted therapy標靶療法中的合成小分子:many are TK inhibitors or ~nibs : small molecules permeable to membrane inhibiting receptor's kinase ( ie. tyrosine kinase ) in the cytoplasm[]

main article: Synthetic small molecule in targeted therapy標靶療法中的合成小分子

unconjugated Synthetic small molecule(many are ~nib)[]

TKI[]

TKI

Serine/threonine kinase inhibitors (small molecules)[]

others[]

  • The selective estrogen receptor modulator tamoxifen has been described as the foundation of targeted therapy.
  • ALK inhibitors, e.g. crizotinib

Small molecule drug conjugates[]

  • Vintafolide is a small molecule drug conjugate consisting of a small molecule targeting the folate receptor. It is currently in clinical trials for platinum-resistant ovarian cancer (PROCEED trial) and a Phase 2b study(TARGET trial) in non-small-cell lung carcinoma (NSCLC).[1]

references[]

20170817wiki

  1. ↑ [1]

Immunotherapy免疫療法[]

molecular Immunotherapy[]

a kind of targeted therapy

cellular Immunotherapy[]

CARTs

Gene therapy(基因療法)[]

Gene therapy(基因療法)

traditional classification[]

Chemotherapy:Alkylating agents(化學療法:烷化劑)[]

  • 或稱烷基化劑
  • alkylation through
    • alkylation through carbocation
    • alkylation through radical
  • alkylation at what position
    • interstrand cross-link
    • intrastrand cross-link

Nitrogen mustards[]

aliphatic[]
aromatic[]
micellaneous(其他):[]

Aziridines[]

  • Triethylenemelamine → Thiotepa
  • Triethylenemelamine → Carboquone ← Mitomycin（Antineoplastics - agents from natural products）
     

Nitrosoureas : alkylation through carbocation : 常常脂溶性夠大而可以治療中樞神經癌症[]

chloroethylnitrosourea : O6 or N7 -alkylation of guanine nucleoties[]
  • Methylnitrosoureas → Carmustine → Nimustine
     
  • Methylnitrosoureas → Iomustine → Nimustine
     
不知道[]
  • Nimustine
  • Methylnitrosoureas → Iomustine → Semustine
  • Streptozocin → Ranimustine
  • Ranimustine

Procarbazine and triazenes: O6-methylation of guanine nucleoties with thymine→MMS(mis match repair system )[]

Procarbazine[]

Procarbazine→diazene intermediate : alkylation through radical

triazenes /Prodrug of MTIC : alkylation through carbocation[]

Alkyl sulfonate[]

  • Busulfan : N7-methylation of guanine nucleoties

organoplatinum/Platinum coordination complex[]

  • Cisplatin(生理食鹽水當作溶劑) N7-methylation of guanine nucleoties → Carboplatin → Nedaplatin
     
  • Carboplatin(D5W當作溶劑) intrastrand cross-link between G and G
  • Nedaplatin
  • Cisplatin → Iproplatin
  • Oxaliplatin

altratamine[]

altratamine:

Cytotoxic antibiotics抗生素[]

Toxic Food食物[]

Chemotherapy:Antimetabolic agents(化學療法:抗代謝)[]

indirect inhibitor of thymidylate synthase (Folic acid antagonists)[]

direct inhibitor of thymidylate synthase : Pyrimidine analogue[]

Purine antagonists : amidophosphoribosyl transferase inhibitors[]

DNA polymerase/DNA chain elongation inhibitor[]

Pyrimidine analogue[]
Purine analogue : adenosine analogue[]

Others[]

Chemotherapy:antibiotics(化學療法:抗生素)(破壞DNA)[]

alkylating agents(烷化劑)[]

radical[]

topoiisomerase Ⅱ inhibitor and radical[]

Topoisomerase Ⅱ inhibitor[]

Anthracyclines ( or Anthraquinone) and anthracenediones[]

屬於抗生素抗癌藥，結構類似tetracycline。2016NEJS臨床藥學- 報告用大圖：DOXORUBICIN引起的心毒性 DOXORUBICIN-INDUCED CARDIOTOXICITY

anthracenediones[]

其他[]

  • menogaril
  • Plicamycin(mithramycin)
  • acivicin
  • anthramycin
  • Pentostatin(2'-deoxycoformycin)(DCF)
  • calicheamicin
  • Peplomycin

Chemotherapy:Agents from natural products=antibiotics+resin+alkaloids(化學療法:天然物=抗生素+樹脂+生物鹼)[]

alkylating agents(烷化劑)[]

radical[]

topoiisomerase Ⅱ inhibitor and radical[]

Topoisomerase Ⅱ inhibitor[]

Anthracyclines ( or Anthraquinone) and anthracenediones[]

屬於抗生素抗癌藥，結構類似tetracycline。

anthracenediones[]
Epipodophyllotoxins[]

屬於普達非倫衍生物，主要抑制topoisomerase Ⅱ。

Topoisomerase Ⅰ inhibitor（Camptothecins）[]

屬於喜樹鹼衍生物，主要抑制topoisomerase Ⅰ。

micellaneous(其他抗生素)[]

  • menogaril
  • Plicamycin(mithramycin)
  • acivicin
  • anthramycin
  • Pentostatin(2'-deoxycoformycin)(DCF)
  • calicheamicin
  • Peplomycin

Antimitotic[]

抑制有絲分裂

Epipodophyllotoxins[]

屬於普達非倫衍生物，主要抑制topoisomerase Ⅱ。

marine natural product halichondrin B[1][2] from Halichondria genus of sponges[3][4][]
  • Eribulin :為抗有絲分裂-a fully synthetic macrocyclic ketone analogue[1][2].
    • cytotoxic mechanisms of action: apoptosis of cancer cells is induced following prolonged and irreversible mitotic blockade.[5][6]
    • non-cytotoxic mechanisms of action:These non-mitotic mechanisms include vascular remodeling that leads to increased tumor perfusion and mitigation of tumor hypoxia, phenotypic changes consistent with reversal of epithelial-mesenchymal transition (EMT), and decreased capacity for migration and invasion leading to reduced metastatic capacity as measured in a preclinical experimental metastasis model.[7][8] In other studies, eribulin treatment of leiomyosarcoma and liposarcoma cells leads to increased expression of smooth muscle and adipocyte differentiation antigens, respectively.[9]
Enhancement of tubulin polymerization（Taxans紫杉醇）[]

促進聚合作用（與生物鹼抗癌藥不同）。

Tubulin polymerization inhibitor（Colchicine & Vinca alkaloids）[]

抑制聚合作用，生物鹼，Colchicine&長春花，屬於indole類，外滲熱敷，使用玻璃酸酶解毒。

other[]

Estramustine

Biologic response modifiers[]

Male Breast carcinoma[]

testosterone

antiprogestin[]

mifepristone(RU486): treat progestone sensitive cancer，但無法治療攝護腺癌

Prostatic carcinoma[]

Progestin[]
  • Chlormadinone acetate（Progestin）
Estrogen[]
Antiandorogens[]
Corticoids inhibitor[]
GnRH agonist[]
  • Goserelin
  • Leuprolide
  • Triptoralen
GnRH antagonist[]
  • abarelix

Breast carcinoma[]

Andorogen[]
  • Fluoxymesterone
Progesterone receptor agonist（Progestins）[]
Corticoids inhibitor[]
Antiestrogens (SERM(slective estrogen receptor modulator))[]
Aromatase inhibitor[]
  • Testolactone
  • Letrozole
  • Anastrozole
  • Fadrozole
  • Exemestane

Leukemia（Glucocorticoids）[]

Thyroid carcinoma（Thyroid hormones）[]

retinoid[]

immunotherapy免疫療法:好站介紹:卡斯柏的癌症免疫治療經驗分享[]

  • Bacillus Calmette-Guerin(BCG)卡介苗
  • interferon
    • interferon alpha-2a
    • interferon alpha-2b
    • interferon alpha-n3
  • aldesleukin
  • denileukin diftitox(Ontak)
  • levamisole
  • thalidominde: treat 多發性骨髓瘤
  • 胰臟癌新療法活化免疫系統 更新日期:2011/04/01 11:35【24drs.com】
  • 當然，癌症是不會傳染的，它們是身體細胞經過某些特定的遺傳和突變而產生。即使如此，免疫系統應該能識別惡性細胞，因為它們表現出異常的分子片段，T細胞和B細胞應該會視其為外來物。然而，由於各種原因，免疫系統有時無法有效對抗癌症。這些年來，在強化免疫反應的努力獲得好壞參半的結果。近來，採用不同的策略已獲取更為一致的成功。事實證明，癌症有時會選擇關閉免疫系統的開關，積極抑制免疫系統對其生長擴張有所反應，而新的療法正是試圖移除這些煞車器。摘自: 召喚免疫軍團來抗癌！ sa.ylib.com/MagCont.aspx?PageIdx=1&Unit=featurearticles&Cate=&id=2444&year=

Photodynamic therapy(PDT)[]

profimer sodium

micellaneous(未歸類)[]

Ethylenimines

Methylmelamines

Uracil mustard

mitotane

L-asaparaginase

pipobroman

amsacrine : 先嵌入DNA

suramin sodium

Gene therapy(基因療法)[]

基因療法:未來醫學 發展的重要方向之ㄧ，把正常的基因送到有疾病的人體內使之基因恢復正常而治療疾病，主要的問題在於:所送入的正常基因如何到達所需送達細胞之DNA的所欲送達位置，如果這個問題能解決，癌症、先天性缺陷等各種無法根治的疾病將可以被根治。解決這個問題的人得諾貝爾醫學獎絕對沒有問題，而且還可以賺大錢.

Targeted therapy(標靶藥物)[]

monoclonal antibody:bind to receptor[]

:Synthetic small molecule in targeted therapy標靶療法中的合成小分子:TK inhibitor: small molecules permeable to membrane inhibiting receptor's kinase ( ie. tyrosine kinase ) in the cytoplasm[]

相關新聞[]

  • 將研擬用於放寬包括降血脂藥物、乳癌標靶藥物「賀延平」、肺癌標靶藥物「艾瑞莎」、胃腸道基質瘤標靶藥物「基利克」、B、C肝炎及H1N1新型流感治療用藥等藥物之使用標準，目前為肺癌第二線標靶藥物的「艾瑞莎」等藥品，可望調整為第一線用藥，「基利克」更為「高貴」藥物第4名，民眾可望減輕自費買藥負擔。
    • 乳癌標靶藥物「賀延平」、
    • 肺癌標靶藥物「艾瑞莎」目前為肺癌第二線標靶藥物的「艾瑞莎」等藥品，可望調整為第一線用藥、
    • 胃腸道基質瘤標靶藥物「基利克」，「基利克」更為「高貴」藥物第4名，民眾可望減輕自費買藥負擔。

New Taiwanese Antineoplastics classification[]

P 20170816 222021 vHDR Auto

relation between antineoplastic, targeted therapy, ~mab,small molecule in targeted therapy and immunotherapy.

P 20170816 222036 vHDR Auto

relations between targeted therapy、immunotherapyand Biological preparation.

增強防禦因子(increase immunity)[]

阻斷癌細胞關起免疫系統(block cancer cell to close immune system)[]

Checkpoint inhibitors檢查點抑制劑: PD-1 I:a targeted therapy, a molecular immunotherapy

刺激免疫系統對癌細胞的辨認(stimulate immune system to recognize cancer cell)[]

雙特異性抗體（bispecific antibodies）:a targeted therapy, a molecular immunotherapy

使T細胞能辨認癌細胞(let T-cell can recognize cancer cell)[]

降低攻擊因子(suppress tumor growth)[]

chemotherapy[]

Chemotherapy:Alkylating agents(化學療法:烷化劑)[]
  • 或稱烷基化劑
  • alkylation through
    • alkylation through carbocation
    • alkylation through radical
  • alkylation at what position
    • interstrand cross-link
    • intrastrand cross-link
Nitrogen mustards[]
=aliphatic=[]
=aromatic=[]
=micellaneous(其他):=[]
Aziridines[]
  • Triethylenemelamine → Thiotepa
  • Triethylenemelamine → Carboquone ← Mitomycin（Antineoplastics - agents from natural products）
Nitrosoureas : alkylation through carbocation : 常常脂溶性夠大而可以治療中樞神經癌症[]
=chloroethylnitrosourea : O6 or N7 -alkylation of guanine nucleoties =[]
  • Methylnitrosoureas → Carmustine → Nimustine
  • Methylnitrosoureas → Iomustine → Nimustine
=不知道=[]
  • Nimustine
  • Methylnitrosoureas → Iomustine → Semustine
  • Streptozocin → Ranimustine
  • Ranimustine
Procarbazine and triazenes: O6-methylation of guanine nucleoties with thymine→MMS(mis match repair system )[]
= Procarbazine =[]

Procarbazine→diazene intermediate : alkylation through radical

= triazenes /Prodrug of MTIC : alkylation through carbocation =[]
Alkyl sulfonate[]
  • Busulfan : N7-methylation of guanine nucleoties
organoplatinum/Platinum coordination complex[]
  • Cisplatin(生理食鹽水當作溶劑) N7-methylation of guanine nucleoties → Carboplatin → Nedaplatin
  • Carboplatin(D5W當作溶劑) intrastrand cross-link between G and G
  • Nedaplatin
  • Cisplatin → Iproplatin
  • Oxaliplatin
altratamine[]

altratamine:

Cytotoxic antibiotics抗生素[]
Toxic Food食物[]
Chemotherapy:Antimetabolic agents(化學療法:抗代謝)[]
indirect inhibitor of thymidylate synthase (Folic acid antagonists)[]
direct inhibitor of thymidylate synthase : Pyrimidine analogue[]
Purine antagonists : amidophosphoribosyl transferase inhibitors[]
DNA polymerase/DNA chain elongation inhibitor[]
=Pyrimidine analogue=[]
=Purine analogue : adenosine analogue=[]
Others[]
Chemotherapy:antibiotics(化學療法:抗生素)(破壞DNA)[]
alkylating agents(烷化劑)[]
radical[]
topoiisomerase Ⅱ inhibitor and radical[]
Topoisomerase Ⅱ inhibitor[]
= Anthracyclines ( or Anthraquinone) and anthracenediones=[]

屬於抗生素抗癌藥，結構類似tetracycline。2016NEJS臨床藥學- 報告用大圖：DOXORUBICIN引起的心毒性 DOXORUBICIN-INDUCED CARDIOTOXICITY

= anthracenediones =[]
其他[]
  • menogaril
  • Plicamycin(mithramycin)
  • acivicin
  • anthramycin
  • Pentostatin(2'-deoxycoformycin)(DCF)
  • calicheamicin
  • Peplomycin
Chemotherapy:Agents from natural products=antibiotics+resin+alkaloids(化學療法:天然物=抗生素+樹脂+生物鹼)[]
alkylating agents(烷化劑)[]
radical[]
topoisomerase Ⅱ inhibitor and radical[]
Topoisomerase Ⅱ inhibitor[]
= Anthracyclines ( or Anthraquinone) and anthracenediones=[]

屬於抗生素抗癌藥，結構類似tetracycline。

= anthracenediones =[]
= Epipodophyllotoxins =[]

屬於普達非倫衍生物，主要抑制topoisomerase Ⅱ。

Topoisomerase Ⅰ inhibitor（Camptothecins）[]

屬於喜樹鹼衍生物，主要抑制topoisomerase Ⅰ。

micellaneous(其他抗生素)[]
  • menogaril
  • Plicamycin(mithramycin)
  • acivicin
  • anthramycin
  • Pentostatin(2'-deoxycoformycin)(DCF)
  • calicheamicin
  • Peplomycin
Antimitotic[]

抑制有絲分裂

= Epipodophyllotoxins =[]

屬於普達非倫衍生物，主要抑制topoisomerase Ⅱ。

=marine natural product halichondrin B[1][2] from Halichondria genus of sponges[3][4] =[]
  • Eribulin :為抗有絲分裂-a fully synthetic macrocyclic ketone analogue[1][2].
    • cytotoxic mechanisms of action: apoptosis of cancer cells is induced following prolonged and irreversible mitotic blockade.[5][6]
    • non-cytotoxic mechanisms of action:These non-mitotic mechanisms include vascular remodeling that leads to increased tumor perfusion and mitigation of tumor hypoxia, phenotypic changes consistent with reversal of epithelial-mesenchymal transition (EMT), and decreased capacity for migration and invasion leading to reduced metastatic capacity as measured in a preclinical experimental metastasis model.[7][8] In other studies, eribulin treatment of leiomyosarcoma and liposarcoma cells leads to increased expression of smooth muscle and adipocyte differentiation antigens, respectively.[9]
= Enhancement of tubulin polymerization（Taxans紫杉醇） =[]

促進聚合作用（與生物鹼抗癌藥不同）。

= Tubulin polymerization inhibitor（Colchicine & Vinca alkaloids） =[]

抑制聚合作用，生物鹼，Colchicine&長春花，屬於indole類，外滲熱敷，使用玻璃酸酶解毒。

=other=[]

Estramustine

targeted therapy[]

unconjugated monoclonal antibody:腫瘤特異性抗體（tumor-specific antibody）-針對特定標靶的未接合型單株抗體，最初的targeted therapy MoAb屬此類[]
  • unconjugated monoclonal antibody:腫瘤特異性抗體（tumor-specific antibody）
    • 針對特定標靶的未接合型單株抗體，最初的targeted therapy MoAb屬此類。
單株抗體偶聯物（Antibody conjugates）[]
    • 抗體藥物複合體/單株抗體藥品偶聯物（Antibody-drug conjugates）、單株抗體結合毒殺藥物（antibody-drug conjugates, ADCs）
    • 放射免疫治療（radioimmunotherapy）=單株抗體放射性同位素偶聯物（antibody-radionuclide conjugates, ARCs）
unconjugated Synthetic small molecule(many are ~nib)[]
Small molecule drug conjugates[]
  • Vintafolide is a small molecule drug conjugate consisting of a small molecule targeting the folate receptor. It is currently in clinical trials for platinum-resistant ovarian cancer (PROCEED trial) and a Phase 2b study(TARGET trial) in non-small-cell lung carcinoma (NSCLC).[10]

Ab-chemotherapeutic conjugates:targeted therapy[]

.

Photodynamic therapy(PDT)[]

profimer sodium

miscellaneous(未歸類)[]

Ethylenimines

Methylmelamines

Uracil mustard

mitotane

L-asaparaginase

pipobroman

amsacrine : 先嵌入DNA

suramin sodium

抑制癌細胞轉移(metastasis inhibitor癌症轉移抑制劑 )[]

natural[]

  • metastasis suppressor

artificial[]

修復突變的基因(replace mutated gene)-Gene therapy(基因療法)[]

基因療法:未來醫學 發展的重要方向之ㄧ，把正常的基因送到有疾病的人體內使之基因恢復正常而治療疾病，主要的問題在於:所送入的正常基因如何到達所需送達細胞之DNA的所欲送達位置，如果這個問題能解決，癌症、先天性缺陷等各種無法根治的疾病將可以被根治。解決這個問題的人得諾貝爾醫學獎絕對沒有問題，而且還可以賺大錢.

未整理完[]

Biologic response modifiers[]

Male Breast carcinoma[]

testosterone

antiprogestin[]

mifepristone(RU486): treat progestone sensitive cancer，但無法治療攝護腺癌

Prostatic carcinoma[]

Progestin[]
  • Chlormadinone acetate（Progestin）
Estrogen[]
Antiandorogens[]
Corticoids inhibitor[]
GnRH agonist[]
  • Goserelin
  • Leuprolide
  • Triptoralen
GnRH antagonist[]
  • abarelix

Breast carcinoma[]

Andorogen[]
  • Fluoxymesterone
Progesterone receptor agonist（Progestins）[]
Corticoids inhibitor[]
Antiestrogens (SERM(slective estrogen receptor modulator))[]
Aromatase inhibitor[]
  • Testolactone
  • Letrozole
  • Anastrozole
  • Fadrozole
  • Exemestane

Leukemia（Glucocorticoids）[]

Thyroid carcinoma（Thyroid hormones）[]

retinoid[]

immunotherapy免疫療法:好站介紹:卡斯柏的癌症免疫治療經驗分享[]

  • Bacillus Calmette-Guerin(BCG)卡介苗
  • interferon
    • interferon alpha-2a
    • interferon alpha-2b
    • interferon alpha-n3
  • aldesleukin
  • denileukin diftitox(Ontak)
  • levamisole
  • thalidominde: treat 多發性骨髓瘤
  • 胰臟癌新療法活化免疫系統 更新日期:2011/04/01 11:35【24drs.com】
  • 當然，癌症是不會傳染的，它們是身體細胞經過某些特定的遺傳和突變而產生。即使如此，免疫系統應該能識別惡性細胞，因為它們表現出異常的分子片段，T細胞和B細胞應該會視其為外來物。然而，由於各種原因，免疫系統有時無法有效對抗癌症。這些年來，在強化免疫反應的努力獲得好壞參半的結果。近來，採用不同的策略已獲取更為一致的成功。事實證明，癌症有時會選擇關閉免疫系統的開關，積極抑制免疫系統對其生長擴張有所反應，而新的療法正是試圖移除這些煞車器。摘自: 召喚免疫軍團來抗癌！ sa.ylib.com/MagCont.aspx?PageIdx=1&Unit=featurearticles&Cate=&id=2444&year=

see also[]

延伸學習[]

reference[]

  1. ↑ 1.0 1.1 1.2 1.3 模板:Cite journal
  2. ↑ 2.0 2.1 2.2 2.3 模板:Cite book
  3. ↑ 3.0 3.1 模板:Cite journal
  4. ↑ 4.0 4.1 模板:Cite journal
  5. ↑ 5.0 5.1 模板:Cite journal
  6. ↑ 6.0 6.1 模板:Cite journal
  7. ↑ 7.0 7.1 模板:Cite journal
  8. ↑ 8.0 8.1 模板:Cite journal
  9. ↑ 9.0 9.1 模板:Cite journal
  10. ↑ [2]
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