卡非佐米的临床研究及应用
摘要
20S蛋白酶体是治疗肿瘤的重要靶点,卡非佐米是针对这一靶点的上市药物,主要用于多发性骨髓瘤的治疗。近年来,随着卡非佐米在临床上的广泛应用,在临床效果、临床安全性、联合应用等方面出现了不同的改变。除此之外,卡非佐米不仅可以治疗骨髓瘤,在乳腺癌、甲状腺未分化癌、多形性胶质母细胞瘤、套细胞瘤、肝细胞癌等疾病上也表现了良好的活性。本文主要从卡非佐米的吸收、分布、代谢、排泄等方面介绍其药代动力学性质。
引文
1 Wayne H,Chase M,Chandler D,et al. Crystal structure of the human20 S proteasome in complex with carfilzomib[J]. CorresMark,2015,23(2):418-424
2 Xiaozhou Z,Alaknanda A,Andrew G T,et al. New peptidomimetic boronates for selective inhibition of the chymotrypsin-like activity of the26 S proteasome[J]. ACS Medicinal Chemistry Letters,2016,7(12):1039-1043
3 Salvini M,Troia R,Giudice D,et al. Pharmacokinetic drug evaluation of ixazomib citrate for the treatment of multiple myeloma[J]. Expert Opinion on Drug Metabolism&Toxicology,2018,14(1):91-99
4 Emilie G,Michele R R,Joelle V. Proteasome inhibitors:recent advances and new perspectives in medicinal chemistry[J]. Current Topics in Medicinal Chemistry,2010,10(3):232-256
5 邢志佳,张叶叶,马宇衡,等.针对20S蛋白酶体的抗肿瘤药物研究进展[J].天津药学,2015,27(1):55-57
6 马李洁,李莉娟,张连生,等.多发性骨髓瘤治疗现状及前景[J].临床荟萃,2015,30(4):476-480
7 马勇,汪兴洪.多发性骨髓瘤治疗进展[J].亚太传统医药,2012,8(4):201-202
8 霍秀颖,封宇飞.蛋白酶体抑制剂卡非佐米的药理作用与临床评价[J].中国新药杂志,2013,22(13):1479-1482
9 韩梅,葛明.治疗多发性骨髓瘤新药———卡非佐米[J].医药导报,2013,32(9):1200-1202
10 Zhengping W,Jinfu Y,Christopher K,et al. Clinical pharmacokinetics,metabolism,and drug-drug interaction of carfilzomib[J]. Drug Metabolism And Disposition,2013,41(4):230-237
11 Jinfu Y,Zhengping W,Ying F,et al. pharmacokinetics,pharmacodynamics,metabolism,distribution,and excretion of carfilzomib in rats[J]. Drug Metabolism And Disposition,2011,39(10):1873-1882
12 陈小燕,张建中,倪海华,等.卡非佐米的药理学及临床研究进展[J].中国抗生素杂志,2015,40(9):717-720
13 Wang H,Guan F G,Chen D,et al. An analysis of the safety profile of proteasome inhibitors for treating various cancers[J]. Expert Opinion on Drug Safety,2014,13(8):1043-1054
14 Usmani S Z,Weiss B M,Plesner T,et al. Clinical efficacy of daratumumab monotherapy in patients with heavily pretreated relapsed or refractory multiple myeloma[J]. Blood,2016,128(1):37-44
15 David S S,Thomas M,Michael W,et al. A phase 2 study of single-agent carfilzomib(PX-171-003-A1)in patients with relapsed and refractory multiple myeloma[J]. Blood,2012,120(4):2817-2825
16 Kim G Y,Ahuja T,Papadopoulos J,et al. Cardiotoxicity with carfilzomib at doses greater than 27 mg/m2:A case series[J]. Oncology Pharmacy Practice,2017,25(1):229-233
17 Brown J,Plummer R,Bauer T M,et al. Pharmacokinetics of carflzomib in patients with advanced malignancies and varying degrees of hepatic impairment:an open-label,single-arm,phase 1 study[J]. Experimental Hematology&Oncology,2017,6(27):1-12
18 Eli M,Morie A G,Hila M. A practical review on carfilzomib in multiple myeloma[J]. European Journal of Haematology,2016,96(6):564-577
19 Shinsuke I,Kensei T,Masafumi T,et al. Phase I dose escalation study of high dose carflzomib monotherapy for Japanese patients with relapsed or refractory multiple myeloma[J]. Cross Mark,2016,104(5):596-604
20 Herv'e A L,Rafael F,David S,et al. Carfilzomib significantly improves the progression-free survival of high-risk patients in multiple myeloma[J]. Blood,2016,128(9):1174-1180
21 Clemens J,Welti L,Weiss J,et al. Bortezomib,carfilzomib and ixazomib do not mediate relevant transporter-based drug-drug interactions[J]. Oncology letters,2017,14(3):3185-3192
22 Kraus M,Bader J,Geurink P P,et al. The novelβ2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells[J]. Haematologica,2015,100(10):1350-1360
23 Liping L,Ningning Z,Wenjun X,et al. Pooled analysis of the reports of carfilzomib,panobinostat,and elotuzumab combinations in patients with refractory/relapsed multiple myeloma[J]. Journal of Hematology&Oncology,2016,9(54):1-7
24 Chen Y,Ooi M,Lim S F,et al. Thrombotic microangiopathy during carfilzomib use:case series in Singapore[J]. Blood Cancer Journal,2016,6(450):1-2
25 James R B,Alan C,Alberto B,et al. CHAMPION-1:a phase 1/2study of once-weekly carfilzomib and dexamethasone for relapsed or refractory multiple myeloma[J]. Blood,2016,127(26):3360-3368
26 Maruyama D,Tobinai K,Chou T,et al. Weekly carfilzomib and dexamethasone in Japanese patients with relapsed or refractory multiple myeloma:A phase 1 and PK/PD trial[J]. Cancer Science,2018,109(10):3245-3252
27 Lin Z,Xiaoxuan J,Shuting H,et al. Analysis of the efficacy and safety of carfilzomib and its combination in multiple myeloma[J]. Journal of Chinese Pharmaceutical Sciences,2017,26(3):222-229
28 Chari A,Larson S,Holkova B,et al. Phase 1 trial of ibrutinib and carfilzomib combination therapy for relapsed or relapsed and refractory multiple myeloma[J]. Leukemia&Lymphoma,2018,59(11):2588-2594
29 Steiner R E,Manasanch E E. Carflzomib boosted combination therapy for relapsed multiple myeloma[J]. Onco Targets and therapy,2017,10:895-907
30 Sophia D,Martin S,Leo R,et al.‘Real-life’experience of preapproval carfilzomib-based therapy in myeloma-analysis of cardiac toxicity and predisposing factors[J]. European Journal of Haematology,2016,97(1):25-32
31 Brian B H,Daywin P,Xing W. molecular mechanisms of the cardiotoxicity of the proteasomal targeted drugs bortezomib and carfilzomib[J].Cardiovasc Toxicol,2017,17(3):237-250
32 Vosgha H,Ariana A,Smith R,et al. miR-205 targets angiogenesis&EMT concurrently in anaplastic thyroid carcinoma[J]. Endocr Relat Cancer,2018,25(3):323-337
33 Amit M,Lisa Z,Myriem B,et al. Carfilzomib is an effective anticancer agent in anaplastic thyroid cancer[J]. Endocrine-Related Cancer,2015,(22):319-329
34 Lisa Z,Myriem B,Ross L,et al. Carflzomib potentiates CUDC-101-induced apoptosis in anaplastic thyroid cancer[J]. Oncotarget,2016,7(13):16517-16528
35 Yonghua S,Yang Y,Zhenyu W,et al. Second-generation proteasome inhibitor carflzomib enhances doxorubicin-induced cytotoxicity and apoptosis in breast cancer cells[J]. Oncotarget,2016,7(45):73697-73710
36 Vyas D,Lopezhisijos N,Shah P,et al. A second-generation proteasome inhibitor and doxorubicin modulates IL-6,pSTAT-3 and NFkB Activity in MDA-MB-231 breast cancer cells[J]. Journal of Nanoscience&Nanotechnology,2017,17(1):175
37 Wang H,Yu J,Wang X,et al. The RNA helicase DHX33 is required for cancer cell proliferation in human glioblastoma and confers resistance to PI3K/m TOR inhibition[J]. Cellular Signalling,2019,54:170-178
38 Areeb Z,Stylli S S,Ware T M B,et al. Inhibition of glioblastoma cell proliferation,migration and invasion by the proteasome antagonist carfilzomib[J]. Cross Mark,2016,33(53):1-8
39 Klener P,Fronkova E,Kalinova M,et al. Potential loss of prognostic significance of minimal residual disease assessment after R-CHOP based induction in elderly patients with mantle cell lymphoma in the era of rituximab maintenance[J]. Hematological Oncology,2018,36(5):773-778
40 Nunes A T,Annunziata C M. Proteasome inhibitors:structure and function[J]. Elsevier,2018,44(6):377-380
41 Zhang L,Pham L V,Newberry K G,et al. In vitro and in vivo therapeutic efficacy of carfilzomib in mantle cell lymphoma:Targeting the Immunoproteasome[J]. Molecular Cancer Therapeutics,2013,12(11):2494-2504
42 Dasmahapatra G,Lembersky D,Son M P,et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells In vitro and in vivo[J]. Molecular Cancer Therapeutics,2011,10(9):1686-1697
43 Mansour M A,Aljoufi M A,Al-Hosaini K,et al. A possible antineoplastic potential of selective,irreversible proteasome inhibitor,carfilzomib on chemically induced hepatocarcinogenesis in rats[J]. Biochemical&Molecular Toxicology,2015,28(9):400-406
44 Mansour M A,Aljoufi M A,Al-Hosaini K,et al. Possible role of selective,irreversible,proteasome inhibitor(carfilzomib)in the treatment of rat hepatocellular carcinoma[J]. Chemico-Biological Interactions,2014,215:17-24
45 Alanazi A,Algfeley S G,Al-Hosaini K A,et al. Therapeutic potential of carfilzomib,an irreversible proteasome inhibitor,against acetaminophen-induced hepatotoxicity in mice[J]. Journal of Biochemical&Molecular Toxicology,2016,31(4):1-5
2 Xiaozhou Z,Alaknanda A,Andrew G T,et al. New peptidomimetic boronates for selective inhibition of the chymotrypsin-like activity of the26 S proteasome[J]. ACS Medicinal Chemistry Letters,2016,7(12):1039-1043
3 Salvini M,Troia R,Giudice D,et al. Pharmacokinetic drug evaluation of ixazomib citrate for the treatment of multiple myeloma[J]. Expert Opinion on Drug Metabolism&Toxicology,2018,14(1):91-99
4 Emilie G,Michele R R,Joelle V. Proteasome inhibitors:recent advances and new perspectives in medicinal chemistry[J]. Current Topics in Medicinal Chemistry,2010,10(3):232-256
5 邢志佳,张叶叶,马宇衡,等.针对20S蛋白酶体的抗肿瘤药物研究进展[J].天津药学,2015,27(1):55-57
6 马李洁,李莉娟,张连生,等.多发性骨髓瘤治疗现状及前景[J].临床荟萃,2015,30(4):476-480
7 马勇,汪兴洪.多发性骨髓瘤治疗进展[J].亚太传统医药,2012,8(4):201-202
8 霍秀颖,封宇飞.蛋白酶体抑制剂卡非佐米的药理作用与临床评价[J].中国新药杂志,2013,22(13):1479-1482
9 韩梅,葛明.治疗多发性骨髓瘤新药———卡非佐米[J].医药导报,2013,32(9):1200-1202
10 Zhengping W,Jinfu Y,Christopher K,et al. Clinical pharmacokinetics,metabolism,and drug-drug interaction of carfilzomib[J]. Drug Metabolism And Disposition,2013,41(4):230-237
11 Jinfu Y,Zhengping W,Ying F,et al. pharmacokinetics,pharmacodynamics,metabolism,distribution,and excretion of carfilzomib in rats[J]. Drug Metabolism And Disposition,2011,39(10):1873-1882
12 陈小燕,张建中,倪海华,等.卡非佐米的药理学及临床研究进展[J].中国抗生素杂志,2015,40(9):717-720
13 Wang H,Guan F G,Chen D,et al. An analysis of the safety profile of proteasome inhibitors for treating various cancers[J]. Expert Opinion on Drug Safety,2014,13(8):1043-1054
14 Usmani S Z,Weiss B M,Plesner T,et al. Clinical efficacy of daratumumab monotherapy in patients with heavily pretreated relapsed or refractory multiple myeloma[J]. Blood,2016,128(1):37-44
15 David S S,Thomas M,Michael W,et al. A phase 2 study of single-agent carfilzomib(PX-171-003-A1)in patients with relapsed and refractory multiple myeloma[J]. Blood,2012,120(4):2817-2825
16 Kim G Y,Ahuja T,Papadopoulos J,et al. Cardiotoxicity with carfilzomib at doses greater than 27 mg/m2:A case series[J]. Oncology Pharmacy Practice,2017,25(1):229-233
17 Brown J,Plummer R,Bauer T M,et al. Pharmacokinetics of carflzomib in patients with advanced malignancies and varying degrees of hepatic impairment:an open-label,single-arm,phase 1 study[J]. Experimental Hematology&Oncology,2017,6(27):1-12
18 Eli M,Morie A G,Hila M. A practical review on carfilzomib in multiple myeloma[J]. European Journal of Haematology,2016,96(6):564-577
19 Shinsuke I,Kensei T,Masafumi T,et al. Phase I dose escalation study of high dose carflzomib monotherapy for Japanese patients with relapsed or refractory multiple myeloma[J]. Cross Mark,2016,104(5):596-604
20 Herv'e A L,Rafael F,David S,et al. Carfilzomib significantly improves the progression-free survival of high-risk patients in multiple myeloma[J]. Blood,2016,128(9):1174-1180
21 Clemens J,Welti L,Weiss J,et al. Bortezomib,carfilzomib and ixazomib do not mediate relevant transporter-based drug-drug interactions[J]. Oncology letters,2017,14(3):3185-3192
22 Kraus M,Bader J,Geurink P P,et al. The novelβ2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells[J]. Haematologica,2015,100(10):1350-1360
23 Liping L,Ningning Z,Wenjun X,et al. Pooled analysis of the reports of carfilzomib,panobinostat,and elotuzumab combinations in patients with refractory/relapsed multiple myeloma[J]. Journal of Hematology&Oncology,2016,9(54):1-7
24 Chen Y,Ooi M,Lim S F,et al. Thrombotic microangiopathy during carfilzomib use:case series in Singapore[J]. Blood Cancer Journal,2016,6(450):1-2
25 James R B,Alan C,Alberto B,et al. CHAMPION-1:a phase 1/2study of once-weekly carfilzomib and dexamethasone for relapsed or refractory multiple myeloma[J]. Blood,2016,127(26):3360-3368
26 Maruyama D,Tobinai K,Chou T,et al. Weekly carfilzomib and dexamethasone in Japanese patients with relapsed or refractory multiple myeloma:A phase 1 and PK/PD trial[J]. Cancer Science,2018,109(10):3245-3252
27 Lin Z,Xiaoxuan J,Shuting H,et al. Analysis of the efficacy and safety of carfilzomib and its combination in multiple myeloma[J]. Journal of Chinese Pharmaceutical Sciences,2017,26(3):222-229
28 Chari A,Larson S,Holkova B,et al. Phase 1 trial of ibrutinib and carfilzomib combination therapy for relapsed or relapsed and refractory multiple myeloma[J]. Leukemia&Lymphoma,2018,59(11):2588-2594
29 Steiner R E,Manasanch E E. Carflzomib boosted combination therapy for relapsed multiple myeloma[J]. Onco Targets and therapy,2017,10:895-907
30 Sophia D,Martin S,Leo R,et al.‘Real-life’experience of preapproval carfilzomib-based therapy in myeloma-analysis of cardiac toxicity and predisposing factors[J]. European Journal of Haematology,2016,97(1):25-32
31 Brian B H,Daywin P,Xing W. molecular mechanisms of the cardiotoxicity of the proteasomal targeted drugs bortezomib and carfilzomib[J].Cardiovasc Toxicol,2017,17(3):237-250
32 Vosgha H,Ariana A,Smith R,et al. miR-205 targets angiogenesis&EMT concurrently in anaplastic thyroid carcinoma[J]. Endocr Relat Cancer,2018,25(3):323-337
33 Amit M,Lisa Z,Myriem B,et al. Carfilzomib is an effective anticancer agent in anaplastic thyroid cancer[J]. Endocrine-Related Cancer,2015,(22):319-329
34 Lisa Z,Myriem B,Ross L,et al. Carflzomib potentiates CUDC-101-induced apoptosis in anaplastic thyroid cancer[J]. Oncotarget,2016,7(13):16517-16528
35 Yonghua S,Yang Y,Zhenyu W,et al. Second-generation proteasome inhibitor carflzomib enhances doxorubicin-induced cytotoxicity and apoptosis in breast cancer cells[J]. Oncotarget,2016,7(45):73697-73710
36 Vyas D,Lopezhisijos N,Shah P,et al. A second-generation proteasome inhibitor and doxorubicin modulates IL-6,pSTAT-3 and NFkB Activity in MDA-MB-231 breast cancer cells[J]. Journal of Nanoscience&Nanotechnology,2017,17(1):175
37 Wang H,Yu J,Wang X,et al. The RNA helicase DHX33 is required for cancer cell proliferation in human glioblastoma and confers resistance to PI3K/m TOR inhibition[J]. Cellular Signalling,2019,54:170-178
38 Areeb Z,Stylli S S,Ware T M B,et al. Inhibition of glioblastoma cell proliferation,migration and invasion by the proteasome antagonist carfilzomib[J]. Cross Mark,2016,33(53):1-8
39 Klener P,Fronkova E,Kalinova M,et al. Potential loss of prognostic significance of minimal residual disease assessment after R-CHOP based induction in elderly patients with mantle cell lymphoma in the era of rituximab maintenance[J]. Hematological Oncology,2018,36(5):773-778
40 Nunes A T,Annunziata C M. Proteasome inhibitors:structure and function[J]. Elsevier,2018,44(6):377-380
41 Zhang L,Pham L V,Newberry K G,et al. In vitro and in vivo therapeutic efficacy of carfilzomib in mantle cell lymphoma:Targeting the Immunoproteasome[J]. Molecular Cancer Therapeutics,2013,12(11):2494-2504
42 Dasmahapatra G,Lembersky D,Son M P,et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells In vitro and in vivo[J]. Molecular Cancer Therapeutics,2011,10(9):1686-1697
43 Mansour M A,Aljoufi M A,Al-Hosaini K,et al. A possible antineoplastic potential of selective,irreversible proteasome inhibitor,carfilzomib on chemically induced hepatocarcinogenesis in rats[J]. Biochemical&Molecular Toxicology,2015,28(9):400-406
44 Mansour M A,Aljoufi M A,Al-Hosaini K,et al. Possible role of selective,irreversible,proteasome inhibitor(carfilzomib)in the treatment of rat hepatocellular carcinoma[J]. Chemico-Biological Interactions,2014,215:17-24
45 Alanazi A,Algfeley S G,Al-Hosaini K A,et al. Therapeutic potential of carfilzomib,an irreversible proteasome inhibitor,against acetaminophen-induced hepatotoxicity in mice[J]. Journal of Biochemical&Molecular Toxicology,2016,31(4):1-5