|
Back to products
Browse products
Approved anticancer agents
Anticancer agents in trials
Anticancer agents
in preclinical trials
Anticancer molecular libraries
Other drug agents
Drug intermediates
Bio-reagents and biochemicals
|
MedKoo product information:
Bortezomib
Bortezomib is a dipeptide boronic acid analogue with antineoplastic
activity. Bortezomib reversibly inhibits the 26S proteasome, a large
protease complex that degrades ubiquinated proteins. By blocking the
targeted proteolysis normally performed by the proteasome,
bortezomib disrupts various cell signaling pathways, leading to cell
cycle arrest, apoptosis, and inhibition of angiogenesis.
Specifically, the agent inhibits nuclear factor (NF)-kappaB, a
protein that is constitutively activated in some cancers, thereby
interfering with NF-kappaB-mediated cell survival, tumor growth, and
angiogenesis. In vivo, bortezomib delays tumor growth and enhances
the cytotoxic effects of radiation and chemotherapy. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus).
|
MedKoo Code#: 100100
|
|
Name:
Bortezomib
|
|
CAS#:
179324-69-7
Synonym: Synonym: PS-341.
US brand name: VELCADE. Code names: LDP 341;
MLN341; PS-341.
IUPAC/Chemical name:
((R)-3-methyl-1-((S)-3-phenyl-2-(pyrazine-2-carboxamido)propanamido)butyl)boronic
acid
|
|
Chemical structure
|
Theoretical analysis
|
|

|
MedKoo Code#: 100100
Name: Bortezomib
CAS#: 179324-69-7
Chemical Formula: C19H25BN4O4
Exact Mass: 384.19689
Molecular Weight: 384.24
Elemental Analysis: C, 59.39; H, 6.56; B,
2.81; N, 14.58; O, 16.66
|
|
Availability and price
Bortezomib
(99%) is in stock.
25 mg / $350.00
100 mg / $850.00
For quotation, question,
and order, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer significant discount
for larger quantity order.
|
|
Quality control
data:
Product will be shipped with supporting
analytical data.
|
|
Information about this agent
|
Bortezomib is "indicated" (recommended) for
single-agent use in the treatment of patients with multiple myeloma who
have received at least two prior therapies and are progressing on their
most recent therapy. Clinical investigations have been completed or are
under way to evaluate the safety and efficacy of bortezomib alone or in
combination with chemotherapy in multiple myeloma, both at relapse and
presentation, as well as in other cancer types.
Bortezomib (VELCADE®, formerly PS-341) was approved
for the treatment of patients with relapsed or refractory multiple
myeloma in May 2003 by the US Food and Drug Administration and in April
2004 by the Committee for Proprietary Medicinal Products of the European
Union. In December 2006 the FDA approved Bortezomib for treatment of
mantle cell lymphoma.
Bortezomib binds to the proteasome and does so
"reversibly" (this is a chemical term that means that the bortezomib
molecule can come free under different micro-cellular chemical
conditions.) Normal healthy (non-cancer) cells are not as prone to
damage from this binding after the Bortezomib comes off, as cancer cells
are. Malignant cells suffer a breakdown even after inhibition of the
proteasome for a short time.
According to
http://en.wikipedia.org/wiki/Bortezomib, Bortezomib was originally
synthesized in 1995 (MG-341) at a company called Myogenics, which soon
changed its name to ProScript. After promising preclinical results, the
drug (PS-341) was tested in a small Phase I clinical trial on patients
with multiple myeloma cancer. ProScript ran out of money and was bought
by Leukosite in May 1999. Leukosite in turn was bought by Millennium
Pharmaceuticals in October 1999. At this point in time, the project had
low priority amongst other projects at the company. This changed
significantly when one of the first volunteers to receive the drug in
the clinical trial achieved a complete response and was still alive four
years later. At the time this was a remarkable result. Later clinical
experimentation indicates the possibility of a complete response in 15%
of patients in a similar condition, when treated with bortezomib. In May
2003, seven years after the initial synthesis, bortezomib (Velcade) was
approved in the United States by the Food and Drug Administration (FDA)
for use in multiple myeloma, based on the results from the SUMMIT Phase
II trial.
Recent publication related to this agent:
1. Pandit, Bulbul; Gartel, Andrei L. New potential
anti-cancer agents synergize with bortezomib and ABT-737 against
prostate cancer. Prostate (Hoboken, NJ, United States) (2010), 70(8),
825-833. CODEN: PRSTDS ISSN:0270-4137. AN 2010:795910
2. Sonnemann, Juergen; Gressmann, Stephanie; Becker, Sabine; Wittig,
Susan; Schmudde, Mareike; Beck, James F. The histone deacetylase
inhibitor vorinostat induces calreticulin exposure in childhood brain
tumour cells in vitro. Cancer Chemotherapy and Pharmacology (2010),
66(3), 611-616. CODEN: CCPHDZ ISSN:0344-5704. AN 2010:760155
3. Roccaro, Aldo M.; Sacco, Antonio; Aujay, Monette; Ngo, Hai T.; Azab,
Abdel Kareem; Azab, Feda; Quang, Phong; Maiso, Patricia; Runnels,
Judith; Anderson, Kenneth C.; Demo, Susan; Ghobrial, Irene M. Selective
inhibition of chymotrypsin-like activity of the immunoproteasome and
constitutive proteasome in Waldenstrom macroglobulinemia. Blood (2010),
115(20), 4051-4060. CODEN: BLOOAW ISSN:0006-4971. AN 2010:725333
4. Lecis, D.; Drago, C.; Manzoni, L.; Seneci, P.; Scolastico, C.;
Mastrangelo, E.; Bolognesi, M.; Anichini, A.; Kashkar, H.; Walczak, H.;
Delia, D. Novel SMAC-mimetics synergistically stimulate melanoma cell
death in combination with TRAIL and Bortezomib. British Journal of
Cancer (2010), 102(12), 1707-1716. CODEN: BJCAAI ISSN:0007-0920. AN
2010:710420
5. Zhang, Lidong; Littlejohn, James E.; Cui, Yu; Cao, Xiaobo; Peddaboina,
Chander; Smythe, W. Roy. Characterization of bortezomib-adapted I-45
mesothelioma cells. Molecular Cancer (2010), 9 No pp. given. CODEN:
MCOACG ISSN:1476-4598. AN 2010:665321
6. Brooks, Alan D.; Jacobsen, Kristen M.; Li, Wenqing; Shanker, Anil;
Sayers, Thomas J. Bortezomib Sensitizes Human Renal Cell Carcinomas to
TRAIL Apoptosis through Increased Activation of Caspase-8 in the
Death-Inducing Signaling Complex. Molecular Cancer Research (2010),
8(5), 729-738. CODEN: MCROC5 ISSN:1541-7786. AN 2010:612515
7. Li, Chunyang; Chen, Shuzhen; Yue, Ping; Deng, Xingming; Lonial, Sagar;
Khuri, Fadlo R.; Sun, Shi-Yong. Proteasome Inhibitor PS-341 (Bortezomib)
Induces Calpain-dependent I B Degradation. Journal of Biological
Chemistry (2010), 285(21), 16096-16104. CODEN: JBCHA3 ISSN:0021-9258. AN
2010:608756
8. Bruna, Jordi; Udina, Esther; Ale, Albert; Vilches, Jorge J.; Vynckier,
Ann; Monbaliu, Johan; Silverman, Lee; Navarro, Xavier.
Neurophysiological, histological and immunohistochemical
characterization of bortezomib-induced neuropathy in mice. Experimental
Neurology (2010), 223(2), 599-608. CODEN: EXNEAC ISSN:0014-4886. AN
2010:550282
9. Lee, Sujin; Yagita, Hideo; Sayers, Thomas J.; Celis, Esteban.
Optimized combination therapy using bortezomib, TRAIL and TLR agonists
in established breast tumors. Cancer Immunology Immunotherapy (2010),
59(7), 1073-1081. CODEN: CIIMDN ISSN:0340-7004. AN 2010:541563
10. Grisendi, Giulia; Bussolari, Rita; Cafarelli, Luigi; Petak, Istvan;
Rasini, Valeria; Veronesi, Elena; De Santis, Giorgio; Spano, Carlotta;
Tagliazzucchi, Mara; Barti-Juhasz, Helga; Scarabelli, Laura; Bambi,
Franco; Frassoldati, Antonio; Rossi, Giulio; Casali, Christian; Morandi,
Uliano; Horwitz, Edwin M.; Paolucci, Paolo; Conte, Pier Franco; Dominici,
Massimo. Adipose-Derived Mesenchymal Stem Cells as Stable Source of
Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand Delivery for
Cancer Therapy. Cancer Research (2010), 70(9), 3718-3729. CODEN: CNREA8
ISSN:0008-5472. AN 2010:533421
11. Carozzi, Valentina A.; Chiorazzi, Alessia; Canta, Annalisa; Lapidus,
Rena G.; Slusher, Barbara S.; Wozniak, Krystyna M.; Cavaletti, Guido.
Glutamate carboxypeptidase inhibition reduces the severity of
chemotherapy-induced peripheral neurotoxicity in rat. Neurotoxicity
Research (2010), 17(4), 380-391. CODEN: NURRFI ISSN:1029-8428. AN
2010:520015
12. Luo, Peihua; Lin, Meihua; Lin, Meili; Zhu, Difeng; Wang, Zhen; Shen,
Jingshan; Yang, Bo; He, Qiaojun. Bortezomib induces apoptosis in human
neuroblastoma CHP126 cells. Pharmazie (2010), 65(3), 213-218. CODEN:
PHARAT ISSN:0031-7144. AN 2010:510915
13. Russo, A.; Bronte, G.; Fulfaro, F.; Cicero, G.; Adamo, V.; Gebbia,
N.; Rizzo, S. Bortezomib: a new pro-apoptotic agent in cancer treatment.
Current Cancer Drug Targets (2010), 10(1), 55-67. CODEN: CCDTB9
ISSN:1568-0096. CAN 152:582651 AN 2010:496378
14. Fuchs, Dominik; Daniel, Volker; Sadeghi, Mahmoud; Opelz, Gerhard;
Naujokat, Cord. Salinomycin overcomes ABC transporter-mediated multidrug
and apoptosis resistance in human leukemia stem cell-like KG-1a cells.
Biochemical and Biophysical Research Communications (2010), 394(4),
1098-1104. CODEN: BBRCA9 ISSN:0006-291X. AN 2010:494291
15. Khan, Omar; Fotheringham, Susan; Wood, Victoria; Stimson, Lindsay;
Zhang, Chunlei; Pezzella, Francesco; Duvic, Madeleine; Kerr, David J.;
La Thangue, Nicholas B. HR23B is a biomarker for tumor sensitivity to
HDAC inhibitor-based therapy. Proceedings of the National Academy of
Sciences of the United States of America (2010), 107(14), 6532-6537,
S6532/1-S6532/2. CODEN: PNASA6 ISSN:0027-8424. CAN 152:583400 AN
2010:478505
16. Sung, Bokyung; Ahn, Kwang Seok; Aggarwal, Bharat B. Noscapine, a
Benzylisoquinoline Alkaloid, Sensitizes Leukemic Cells to
Chemotherapeutic Agents and Cytokines by Modulating the NF- B Signaling
Pathway. Cancer Research (2010), 70(8), 3259-3268. CODEN: CNREA8
ISSN:0008-5472. AN 2010:470279
17. Ouyang, Guifang; Lin, Maofang. Combined effects of bortezomib and
daunorubicin on multiple myeloma cell KM3 in vitro. Zhongguo Shiyan
Xueyexue Zazhi (2009), 17(6), 1468-1471. CODEN: ZSXZAF ISSN:1009-2137.
AN 2010:463340
18. Moriuchi, Makiko; Ohmachi, Ken; Kojima, Minoru; Tsuboi, Kosuke;
Ogawa, Yoshiaki; Nakamura, Naoya; Ando, Kiyoshi. Three cases of
bortezomib-resistant multiple myeloma with extramedullary masses. Tokai
Journal of Experimental and Clinical Medicine (2010), 35(1), 17-20.
CODEN: TJEMDR ISSN:0385-0005. AN 2010:453450
19. Rao, Rekha; Nalluri, Srilatha; Kolhe, Ravindra; Yang, Yonghua;
Fiskus, Warren; Chen, Jianguang; Ha, Kyungsoo; Buckley, Kathleen M.;
Balusu, Ramesh; Coothankandaswamy, Veena; Joshi, Atul; Atadja, Peter;
Bhalla, Kapil N. Treatment with Panobinostat Induces Glucose-Regulated
Protein 78 Acetylation and Endoplasmic Reticulum Stress in Breast Cancer
Cells. Molecular Cancer Therapeutics (2010), 9(4), 942-952. CODEN:
MCTOCF ISSN:1535-7163. CAN 152:560313 AN 2010:434958
20. Meregalli, Cristina; Canta, Annalisa; Carozzi, Valentina A.;
Chiorazzi, Alessia; Oggioni, Norberto; Gilardini, Alessandra; Ceresa,
Cecilia; Avezza, Federica; Crippa, Luca; Marmiroli, Paola; Cavaletti,
Guido. Bortezomib-induced painful neuropathy in rats: A behavioral,
neurophysiological and pathological study in rats. European Journal of
Pain (Oxford, United Kingdom) (2010), 14(4), 343-350. CODEN: EJPAFJ
ISSN:1090-3801. AN 2010:434842
21. Genin, E.; Reboud-Ravaux, M.; Vidal, J. Proteasome inhibitors:
recent advances and new perspectives in medicinal chemistry. Current
Topics in Medicinal Chemistry (Sharjah, United Arab Emirates) (2010),
10(3), 232-256. CODEN: CTMCCL ISSN:1568-0266. CAN 152:516315 AN
2010:423458
22. O'Connor, Owen A.; Portlock, Carol; Moskowitz, Craig; Hamlin, Paul;
Straus, David; Gerecitano, John; Gonen, Mithat; Dumitrescu, Otilia;
Sarasohn, Debra; Butos, John; Neylon, Ellen; MacGregor Cortelli,
Barbara; Blumel, Susan; Evens, Andrew M.; Zelenetz, Andrew D.; Wright,
John; Cooper, Brenda; Winter, Jane; Vose, Julie. Time to treatment
response in patients with follicular lymphoma treated with bortezomib is
longer compared with other histologic subtypes. Clinical Cancer Research
(2010), 16(2), 719-726. CODEN: CCREF4 ISSN:1078-0432. AN 2010:419963
23. Paoluzzi, Luca; Scotto, Luigi; Marchi, Enrica; Zain, Jasmine; Seshan,
Venkatraman E.; O'Connor, Owen A. Romidepsin and belinostat synergize
the antineoplastic effect of bortezomib in mantle cell lymphoma.
Clinical Cancer Research (2010), 16(2), 554-565. CODEN: CCREF4
ISSN:1078-0432. AN 2010:419948
24. Haglund, Caroline; Aaleskog, Anna; Hakansson, Lena Douhan; Hoeglund,
Martin; Jacobsson, Stefan; Larsson, Rolf; Lindhagen, Elin. The FMCA-GM
assays, high throughput non-clonogenic alternatives to CFU-GM in
preclinical hematotoxicity testing. Toxicology Letters (2010), 194(3),
102-107. CODEN: TOLED5 ISSN:0378-4274. CAN 152:516424 AN 2010:370092
25. Psallidas, Ioannis; Karabela, Sophia P.; Moschos, Charalampos;
Sherrill, Taylor P.; Kollintza, Androniki; Magkouta, Sophia;
Theodoropoulou, Panagiota; Roussos, Charis; Blackwell, Timothy S.;
Kalomenidis, Ioannis; Stathopoulos, Georgios T. Specific effects of
bortezomib against experimental malignant pleural effusion: a
preclinical study. Molecular Cancer (2010), 9 No pp. given. CODEN:
MCOACG ISSN:1476-4598. AN 2010:368278
26. Albero, M. P.; Vaquer, J. M.; Andreu, E. J.; Villanueva, J. J.;
Franch, L.; Ivorra, C.; Poch, E.; Agirre, X.; Prosper, F.; Perez-Roger,
I. Bortezomib decreases Rb phosphorylation and induces caspase-dependent
apoptosis in Imatinib-sensitive and -resistant Bcr-Abl1-expressing
cells. Oncogene (2010), 29(22), 3276-3286. CODEN: ONCNES ISSN:0950-9232.
CAN 152:560300 AN 2010:366094
27. Campbell, Richard A.; Sanchez, Eric; Steinberg, Jeffrey; Shalitin,
Dror; Li, Zhi-Wei; Chen, Haiming; Berenson, James R. Vorinostat enhances
the antimyeloma effects of melphalan and bortezomib. European Journal of
Haematology (2010), 84(3), 201-211. CODEN: EJHAEC ISSN:0902-4441. AN
2010:335556
28. Petruzziello, Fara; Zeppa, Pio; Catalano, Lucio; Cozzolino,
Immacolata; Gargiulo, Giuseppe; Musto, Pellegrino; D'Auria, Fiorella;
Liso, Vincenzo; Rizzi, Rita; Caruso, Nadia; Califano, Catello; Piro,
Eugenio; Musso, Maurizio; Bonanno, Vincenza; Pia Falcone, Antonietta;
Tafuto, Salvatore; Raimondo, Francesco; Laurentiis, Michelino; Pane,
Fabrizio; Palombini, Lucio; Rotoli, Bruno. Amyloid in bone marrow smears
of patients affected by multiple myeloma. Annals of Hematology (2010),
89(5), 469-474. CODEN: ANHEE8 ISSN:0939-5555. AN 2010:332295
29. Amschler, Katharina; Schoen, Michael P.; Pletz, Nadin; Wallbrecht,
Katrin; Erpenbeck, Luise; Schoen, Margarete. NF- B Inhibition through
Proteasome Inhibition or IKK Blockade Increases the Susceptibility of
Melanoma Cells to Cytostatic Treatment through Distinct Pathways.
Journal of Investigative Dermatology (2010), 130(4), 1073-1086. CODEN:
JIDEAE ISSN:0022-202X. AN 2010:326986
30. Casafont, Inigo; Berciano, Maria T.; Lafarga, Miguel. Bortezomib
induces the formation of nuclear poly(A) RNA granules enriched in Sam68
and PABPN1 in sensory ganglia neurons. Neurotoxicity Research (2010),
17(2), 167-178. CODEN: NURRFI ISSN:1029-8428. AN 2010:321963
31. Dick, Lawrence R.; Fleming, Paul E. \Building on bortezomib:
second-generation proteasome inhibitors as anti-cancer therapy. Drug
Discovery Today (2010), 15(5/6), 243-249. CODEN: DDTOFS ISSN:1359-6446.
AN 2010:318415
32. Koschny, Ronald; Holland, Heidrun; Sykora, Jaromir; Erdal, Hande;
Krupp, Wolfgang; Bauer, Manfred; Bockmuehl, Ulrike; Ahnert, Peter;
Meixensberger, Juergen; Stremmel, Wolfgang; Walczak, Henning; Ganten,
Tom M. Bortezomib sensitizes primary human esthesioneuroblastoma cells
to TRAIL-induced apoptosis. Journal of Neuro-Oncology (2010), 97(2),
171-185. CODEN: JNODD2 ISSN:0167-594X. AN 2010:318328
33. Miller, Susanne C.; Huang, Ruili; Sakamuru, Srilatha; Shukla, Sunita
J.; Attene-Ramos, Matias S.; Shinn, Paul; Van Leer, Danielle; Leister,
William; Austin, Christopher P.; Xia, Menghang. Identification of known
drugs that act as inhibitors of NF- B signaling and their mechanism of
action. Biochemical Pharmacology (2010), 79(9), 1272-1280. CODEN: BCPCA6
ISSN:0006-2952. CAN 152:541287 AN 2010:304337
34. Hagenbuchner, Judith; Ausserlechner, Michael J.; Porto, Verena;
David, Reinhard; Meister, Bernhard; Bodner, Martin; Villunger, Andreas;
Geiger, Kathrin; Obexer, Petra. The Anti-apoptotic Protein BCL2L1/Bcl-xL
Is Neutralized by Pro-apoptotic PMAIP1/Noxa in Neuroblastoma, Thereby
Determining Bortezomib Sensitivity Independent of Prosurvival MCL1
Expression. Journal of Biological Chemistry (2010), 285(10), 6904-6912.
CODEN: JBCHA3 ISSN:0021-9258. CAN 152:397431 AN 2010:252674
35. Kupperman, Erik; Lee, Edmund C.; Cao, Yueying; Bannerman, Bret;
Fitzgerald, Michael; Berger, Allison; Yu, Jie; Yang, Yu; Bruzzese,
Frank; Liu, Jane; Blank, Jonathan; Garcia, Khristofer; Tsu, Christopher;
Dick, Larry; Fleming, Paul; Yu, Li; Manfredi, Mark; Rolfe, Mark; Bolen,
Joe. Evaluation of the Proteasome Inhibitor MLN9708 in Preclinical
Models of Human Cancer. Cancer Research (2010), 70(5), 1970-1980. CODEN:
CNREA8 ISSN:0008-5472. CAN 152:517050 AN 2010:251104
36. Seeger, Jens Michael; Schmidt, Patrick; Brinkmann, Kerstin; Hombach,
Andreas A.; Coutelle, Oliver; Zigrino, Paola; Wagner-Stippich, Diana;
Mauch, Cornelia; Abken, Hinrich; Kroenke, Martin; Kashkar, Hamid. The
Proteasome Inhibitor Bortezomib Sensitizes Melanoma Cells toward
Adoptive CTL Attack. Cancer Research (2010), 70(5), 1825-1834. CODEN:
CNREA8 ISSN:0008-5472. CAN 152:446019 AN 2010:251089
37. Armstrong, Jane L.; Flockhart, Ross; Veal, Gareth J.; Lovat, Penny
E.; Redfern, Christopher P. F. Regulation of endoplasmic reticulum
stress-induced cell death by ATF4 in neuroectodermal tumor cells.
Journal of Biological Chemistry (2010), 285(9), 6091-6100. CODEN: JBCHA3
ISSN:0021-9258. CAN 152:378285 AN 2010:222084
38. Zhu, Yongqiang; Zhu, Xinrong; Wu, Gang; Ma, Yuheng; Li, Yuejie;
Zhao, Xin; Yuan, Yunxia; Yang, Jie; Yu, Sen; Shao, Feng; Li, Runtao; Ke,
Yanrong; Lu, Aijun; Liu, Zhenming; Zhang, Liangren. Synthesis, in vitro
and in vivo biological evaluation, docking studies, and
structure-activity relationship (SAR) discussion of dipeptidyl boronic
acid proteasome inhibitors composed of -amino acids. Journal of
Medicinal Chemistry (2010), 53(5), 1990-1999. CODEN: JMCMAR
ISSN:0022-2623. CAN 152:358291 AN 2010:199697
39. Pedeboscq, Stephane; L'Azou, Beatrice; Passagne, Isabelle; De Giorgi,
Francesca; Ichas, Francois; Liguoro, Dominique; Pometan, Jean-Paul;
Cambar, Jean. Anticancer drugs exert differential apoptotic and
cytotoxic effects on glioblastoma primary cultures with various EGFR and
bcl-2 profiles. Journal of Experimental Therapeutics and Oncology
(2009), 8(2), 105-116. CODEN: JETOFX ISSN:1359-4117. AN 2010:192268
40. Gasparetto, Cristina; Gockerman, Jon P.; Diehl, Louis F.; de Castro,
Carlos M.; Moore, Joseph O.; Long, Gwynn D.; Horwitz, Mitchell E.;
Keogh, George; Chute, John P.; Sullivan, Keith M.; Neuwirth, Rachel;
Davis, Patricia H.; Sutton, Linda M.; Anderson, Russell D.; Chao, Nelson
J.; Rizzieri, David. "Short course" bortezomib plus melphalan and
prednisone as induction prior to transplant or as frontline therapy for
nontransplant candidates in patients with previously untreated multiple
myeloma. Biology of Blood and Marrow Transplantation (2010), 16(1),
70-77. CODEN: BBMTF6 ISSN:1083-8791. AN 2010:191870
41. Ling, Xiang; Calinski, Diane; Chanan-Khan, Asher A.; Zhou, Muxiang;
Li, Fengzhi. Cancer cell sensitivity to bortezomib is associated with
survivin and p53 status but not cancer cell types. Journal of
Experimental & Clinical Cancer Research (2010), 29 No pp. given. CODEN:
JECRDN ISSN:1756-9966. AN 2010:175140
42. Guenterberg, Kristan D.; Grignol, Valerie P.; Raig, Ene T.; Zimmerer,
Jason M.; Chan, Anthony N.; Blaskovits, Farriss M.; Young, Gregory S.;
Nuovo, Gerard J.; Mundy, Bethany L.; Lesinski, Gregory B.; Carson,
William E., III. Interleukin-29 Binds to Melanoma Cells Inducing Jak-STAT
Signal Transduction and Apoptosis. Molecular Cancer Therapeutics (2010),
9(2), 510-520. CODEN: MCTOCF ISSN:1535-7163. CAN 152:451922 AN
2010:173813
43. Thomas, Sheeba K.; Richards, Tiffany A.; Weber, Donna M. Novel
agents for relapsed and/or refractory multiple myeloma. Cancer Journal
(Hagerstown, MD, United States) (2009), 15(6), 485-493. CODEN: CAJOCB
ISSN:1528-9117. AN 2010:171336
44. Chauhan, Dharminder; Singh, Ajita V.; Ciccarelli, Bryan; Richardson,
Paul G.; Palladino, Michael A.; Anderson, Kenneth C. Combination of
novel proteasome inhibitor NPI-0052 and lenalidomide trigger in vitro
and in vivo synergistic cytotoxicity in multiple myeloma. Blood (2010),
115(4), 834-845. CODEN: BLOOAW ISSN:0006-4971. AN 2010:165189
45. Di Bella, Nicholas; Taetle, Raymond; Kolibaba, Kathryn; Boyd,
Thomas; Raju, Robert; Barrera, David; Cochran, Ernest W., Jr.; Dien,
Philip Y.; Lyons, Roger; Schlegel, Peter J.; Vukelja, Svetislava J.;
Boston, Julie; Boehm, Kristi A.; Wang, Yunfei; Asmar, Lina. Results of a
phase 2 study of bortezomib in patients with relapsed or refractory
indolent lymphoma. Blood (2010), 115(3), 475-480. CODEN: BLOOAW
ISSN:0006-4971. AN 2010:153313
46. Benson, Don M., Jr.; Panzner, Kathryn; Hamadani, Mehdi; Hofmeister,
Craig C.; Bakan, Courtney E.; Smith, Megan K.; Elder, Pat; Krugh, David;
O'Donnell, Lynn; Devine, Steven M. Effects of induction with novel
agents versus conventional chemotherapy on mobilization and autologous
stem cell transplant outcomes in multiple myeloma. Leukemia & Lymphoma
(2010), 51(2), 243-251. CODEN: LELYEA ISSN:1042-8194. AN 2010:138845
47. Corso, Alessandro; Barbarano, Luciana; Mangiacavalli, Silvia;
Spriano, Mauro; Alessandrino, Emilio P.; Cafro, Anna Maria; Pascutto,
Cristiana; Varettoni, Marzia; Bernasconi, Paolo; Grillo, Giovanni;
Carella, Angelo M.; Montalbetti, Luigi; Lazzarino, Mario; Morra, Enrica.
Bortezomib plus dexamethasone can improve stem cell collection and
overcome the need for additional chemotherapy before autologous
transplant in patients with myeloma. Leukemia & Lymphoma (2010), 51(2),
236-242. CODEN: LELYEA ISSN:1042-8194. AN 2010:138841
48. Chen, Szu-Ting; Thomas, Simmy; Gaffney, Kevin J.; Louie, Stan G.;
Petasis, Nicos A.; Schoenthal, Axel H. Cytotoxic effects of celecoxib on
Raji lymphoma cells correlate with aggravated endoplasmic reticulum
stress but not with inhibition of cyclooxygenase-2. Leukemia Research
(2010), 34(2), 250-253. CODEN: LEREDD ISSN:0145-2126. AN 2010:135366
49. Dimopoulos, Meletios A.; Richardson, Paul G.; Schlag, Rudolf;
Khuageva, Nuriet K.; Shpilberg, Ofer; Kastritis, Efstathios; Kropff,
Martin; Petrucci, Maria T.; Delforge, Michel; Alexeeva, Julia; Schots,
Rik; Masszi, Tamas; Mateos, Maria-Victoria; Deraedt, William; Liu,
Kevin; Cakana, Andrew; van de Velde, Helgi; San Miguel, Jesus F. VMP (bortezomib,
melphalan, and prednisone) is active and well tolerated in newly
diagnosed patients with multiple myeloma with moderately impaired renal
function, and results in reversal of renal impairment: cohort analysis
of the phase III VISTA study. Journal of Clinical Oncology (2009),
27(36), 6086-6093. CODEN: JCONDN ISSN:0732-183X. AN 2010:122324
50. Lundqvist, Andreas; Su, Su; Rao, Sheila; Childs, Richard. Cutting
edge: bortezomib-treated tumors sensitized to NK cell apoptosis
paradoxically acquire resistance to antigen-specific T cells. Journal of
Immunology (2010), 184(3), 1139-1142. CODEN: JOIMA3 ISSN:0022-1767. CAN
152:303692 AN 2010:105113
Recent patents related
to Bortezomib
1. Gant, Thomas G. Podophyllotoxin inhibitors of
topoisomerase II. U.S. Pat. Appl. Publ. (2010), 70pp. CODEN: USXXCO US
2010143296 A1 20100610 AN 2010:717477
2. Gant, Thomas G.; Sarshar, Sepehr. Preparation of deuterated gefitinib
derivatives as inhibitors of EGFR tyrosine kinase. U.S. Pat. Appl. Publ.
(2010), 41pp. CODEN: USXXCO US 2010143295 A1 20100610 AN 2010:717472
3. Kocherlakota, Chandrasekhar; Nallamothu, Lavanya; Kovoru, Krishnam
Raju; Banda, Nagaraju; Sridhar, Mittapally; Chandrkanth, Keni Devendra;
Shantreddy, Soogareddy Channareddy; Chhagan, Wagh Sanjay; Pillai,
Raviraj Sukumar; Sreedhar, Bandari; Kranthikumar, Hinge. Pharmaceutical
compositions comprising boronic acid compounds. PCT Int. Appl. (2010),
31pp. CODEN: PIXXD2 WO 2010039762 A2 20100408 CAN 152:415376 AN
2010:439679
4. Tang, Weiping; Bradner, James Elliot; Schreiber, Stuart L.
Deacetylase inhibitors for proliferative diseases therapy. PCT Int.
Appl. (2010), 72pp. CODEN: PIXXD2 WO 2010011296 A2 20100128 CAN
152:207088 AN 2010:110311
5. Kalesse, Markus; Malek, Nisar; Frank, Ronald; Brodmann, Tobias;
Buelow, Leila; Rentsch, Andreas; Girbig, Anna-Katharina; Eggert, Ulrike.
Method for producing intermediates for the production of novel
macrocycles that are inhibitors of the proteasomic degradation of p27,
such as argyrin and derivatives thereof, and uses of said macrocycles.
PCT Int. Appl. (2010), 63pp. CODEN: PIXXD2 WO 2010006682 A1 20100121 CAN
152:184292 AN 2010:84637
6. Zhang, Ji; Wang, Kankan; Pan, Xiaoling; Fang, Hai. Fenretinide or
bioactive derivatives and combinations as antitumor agents. U.S. Pat.
Appl. Publ. (2010), 41pp. CODEN: USXXCO US 2010008896 A1 20100114 CAN
152:161008 AN 2010:54639
7. Lawrence, Harshani; Ge, Yiyu; Sebti, Said M.; Guida, Wayne.
Preparation of 2-amino-1,4-naphthoquinones and N-aryl-aromatic
sulfonamides as proteasome inhibitors for selectively inducing apoptosis
in cancer cells. PCT Int. Appl. (2010), 156 pp. CODEN: PIXXD2 WO
2010005534 A2 20100114 CAN 152:144352 AN 2010:51285
8. Kalesse, Markus; Malek, Nisar; Frank, Roland. Method for producing
intermediates for the production of novel macrocycles that are
inhibitors of the proteasomic degradation of p27, such as argyrin and
derivatives thereof, and uses of said macrocycles. Eur. Pat. Appl.
(2009), 43pp. CODEN: EPXXDW EP 2138507 A1 20091230 CAN 152:111660 AN
2009:1617359
9. Carniato, Denis; Jaillardon, Karine; Busnel, Olivier; Gutmann,
Mathieu; Briand, Jean-Francois; Deprez, Benoit; Thomas, Dominique;
Bougeret, Cecile. Preparation of substituted acetamides useful for the
treatment of cancers, especially cancers resistant to chemotherapy. PCT
Int. Appl. (2009), 161pp. CODEN: PIXXD2 WO 2009150248 A1 20091217 CAN
152:75062 AN 2009:1570694
10. Lattuada, Luciano; Cappelletti, Enrico; Linder, Karen E.; Nunn,
Adrian D.; Lantry, Laura. Preparation of gastrin-releasing peptide
compounds for use in diagnostic imaging or therapy. PCT Int. Appl.
(2009), 396pp. CODEN: PIXXD2 WO 2009143101 A2 20091126 CAN 152:12640 AN
2009:1469249
11. Verner, Erik; Balasubramanian, Sriram; Buggy, Joseph J. Preparation
of benzimidazole, indole, azaindole, and pyrrole hydroxyamides as
selective inhibitors of histone deacetylase 8 for treating cancer,
arthritis, and other diseases. PCT Int. Appl. (2009), 176 pp. CODEN:
PIXXD2 WO 2009129335 A2 20091022 CAN 151:470205 AN 2009:1294451
12. Williams, Brian John; Frederickson, Martyn. Preparation of
isoindolyl phenyl methanone derivs. for treating and preventing
HSP90-mediated diseases. PCT Int. Appl. (2009), 153pp. CODEN: PIXXD2 WO
2009125230 A1 20091015 CAN 151:470037 AN 2009:1263402
13. Kuhn, Michael; Campillos, Monica; Bork, Peer; Jensen, Lars Juhl;
Gavin, Anne-Claude; Petsalaki, Evangelia; Garcia Urdales, Eduardo;
Russel, Rob. Pharmaceutically active compounds with novel medical uses
and method of identifying such compounds. PCT Int. Appl. (2009), 161pp.
CODEN: PIXXD2 WO 2009124755 A1 20091015 CAN 151:440606 AN 2009:1263383
14. Masse, Craig E.; Tung, Roger. Preparation of quinazoline derivatives
as inhibitors of cell surface receptor tyrosine kinases for disease
treatment. PCT Int. Appl. (2009), 60pp. CODEN: PIXXD2 WO 2009121042 A1
20091001 CAN 151:403327 AN 2009:1203961
15. Turcotte, Sandra; Chan, Denise A.; Sutphin, Patrick D.; Giaccia,
Amato J.; Hay, Michael P.; Denny, William A.; Bonnet, Muriel Marie.
Preparation of pyridinyl-substituted 1,3-thiazol-2-amine derivatives
useful for the treatment of cancer. PCT Int. Appl. (2009), 255pp. CODEN:
PIXXD2 WO 2009114552 A1 20090917 CAN 151:381337 AN 2009:1137834
16. Garlich, Joseph R.; Durden, Donald L.; Patterson, Mary; Su, Jingdon;
Suhr, Robert G.; Peng, Xiaodong. O-alkylated PI3 kinase inhibitor
prodrug combination. PCT Int. Appl. (2009), 132pp. CODEN: PIXXD2 WO
2009108704 A1 20090903 CAN 151:328859 AN 2009:1080380
17. Birkus, Gabriel; Watkins, William J.; Ray, Adrian S.; Tumas, Daniel.
Preparation of aminoalkoxypurinyl ethoxymethylphosphonic acid
derivatives and their use in treatment of tumors or viral infections.
PCT Int. Appl. (2009), 98 pp. CODEN: PIXXD2 WO 2009105513 A2 20090827
CAN 151:289313 AN 2009:1042140
18. Kato, Tetsuya; Kawanishi, Nobuhiko; Mita, Takashi; Nonoshita,
Katsumasa; Ohkubo, Mitsuru. Preparation of novel aminopyridine
derivatives having Aurora A selective inhibitory action. PCT Int. Appl.
(2009), 107pp. CODEN: PIXXD2 WO 2009104802 A1 20090827 CAN 151:313570 AN
2009:1041368
19. Livney, Yoav David; Assaraf, Yehuda G.; Shapira, Alina. Casein
particles encapsulating therapeutically active agents and uses thereof.
PCT Int. Appl. (2009), 69pp. CODEN: PIXXD2 WO 2009101614 A1 20090820 CAN
151:253990 AN 2009:1014038
20. Elledge, Stephen J.; Luo, Ji; Schlabach, Michael; Solimini, Nicole.
Treatment of cancer using inhibitors of the mitosis regulatory gene
identified by genome-wide RNAi screen for synthetic lethal interactions
with the K-RAS oncogene. PCT Int. Appl. (2009), 358pp. CODEN: PIXXD2 WO
2009099991 A2 20090813 CAN 151:260662 AN 2009:977212
21. Gant, Thomas G. Preparation of substituted oxazaphosphorine and
their biological activity. U.S. Pat. Appl. Publ. (2009), 72pp. CODEN:
USXXCO US 2009202540 A1 20090813 CAN 151:267183 AN 2009:976161
22. Henteman, Martin F.; Scott, William; Wood, Jill; Johnson, Jeffrey;
Redman, Aniko; Bullion, Ann-Marie; Guernon, Leatte. Preparation of
sulfonyldihydroimidazoquinazoline derivatives for use as PIK3
inhibitors. PCT Int. Appl. (2009), 133pp. CODEN: PIXXD2 WO 2009091550 A2
20090723 CAN 151:173483 AN 2009:887413
23. Arbiser, Jack L. Triarylmethane analogs and their use in treating
cancers and other conditions. U.S. Pat. Appl. Publ. (2009), 64pp. CODEN:
USXXCO US 2009176745 A1 20090709 CAN 151:140445 AN 2009:828524
24. Kraus, Elmar; Bruecher, Christoph; Daelken, Benjamin; Zeng, Steffen;
Osterroth, Frank; Uherek, Christoph; Aigner, Silke; Germer, Matthias.
Immunoconjugates targeting CD138. PCT Int. Appl. (2009), 94pp. CODEN:
PIXXD2 WO 2009080830 A1 20090702 CAN 151:116608 AN 2009:797707
25. Daelken, Benjamin; Uherek, Christoph; Anderson, Kenneth; Hideshima,
Teru; Bruecher, Christoph. Immunoconjugates targeting of
CD138-expressing tumor cells. PCT Int. Appl. (2009), 108pp. CODEN:
PIXXD2 WO 2009080832 A1 20090702 CAN 151:116607 AN 2009:797706
26. Ghobrial, Irene; Roccaro, Aldo; Chauhan, Dharminder; Anderson,
Kenneth; Palladino, Michael A. Methods of using [3.2.0] heterocyclic
compounds and analogs thereof in treating Waldenstrom's
macroglobulinemia. U.S. Pat. Appl. Publ. (2009), 62pp. CODEN: USXXCO US
2009156469 A1 20090618 CAN 151:70266 AN 2009:739404
27. preparation of pyrazolotriazines as kinesin Eg5 inhibitors having
antiproliferative and/or apoptosis inducing activity. Eur. Pat. Appl.
(2009), 68pp. CODEN: EPXXDW EP 2070932 A1 20090617 CAN 151:78149 AN
2009:732133
28. Tung, Roger. Preparation of deuterated
phenylpiperazinylpyrimidinylaminothiazolecarboxamide derivatives for use
as kinase inhibitors. U.S. Pat. Appl. Publ. (2009), 19pp. CODEN: USXXCO
US 2009149399 A1 20090611 CAN 151:56863 AN 2009:710362
29. Temtsin Krayz, Galia; Averbuch, Maryana; Gitis, Larisa; Zelkind,
Ilya. Colloidal nanodispersion compositions comprising lipophilic active
compounds and method for their preparation. PCT Int. Appl. (2009), 97pp.
CODEN: PIXXD2 WO 2009040818 A1 20090402 CAN 150:406559 AN 2009:391361
30. Maier, Thomas; Beckers, Thomas; Baer, Thomas; Vennemann, Matthias;
Gekeler, Volker; Zimmermann, Astrid; Gimmnich, Petra; Padiya, Kamlesh
J.; Joshi, Hemant; Joshi, Uday; Makhija, Mahindra. Preparation of novel
fused tetrahydropyridines as inhibitors of histone deacetylases. PCT
Int. Appl. (2009), 346pp. CODEN: PIXXD2 WO 2009037001 A2 20090326 CAN
150:374299 AN 2009:364201
31. Palle, Raghavendracharyulu Venkata; Kadaboina, Rajasekhar; Murki,
Veerender; Manda, Amarendhar; Gunda, Nageshwar; Pulla, Ramaseshagiri Rao;
Hanmanthu, Mallesha; Mopidevi, Narasimha Naidu; Ramdoss, Suresh Kumar.
Preparation of bortezomib in crystalline form. PCT Int. Appl. (2009), 69
pp. CODEN: PIXXD2 WO 2009036281 A2 20090319 CAN 150:330133 AN
2009:333074
32. Zhang, Yuanpeng; Huang, Anthony; Luo, Bing; Wang, Jinkang. Liposome
formulations of peptide boronic acid compounds for tumor treatment. PCT
Int. Appl. (2009), 37pp. CODEN: PIXXD2 WO 2009026430 A2 20090226 CAN
150:268053 AN 2009:239302
33. Mutz, Mitchell W.; Marquis, Andre L. Pharmacokinetics and efficacy
of anti-angiogenic drugs and drugs treating diseases of the blood. U.S.
Pat. Appl. Publ. (2009), 27 pp. CODEN: USXXCO US 2009053245 A1 20090226
CAN 150:275565 AN 2009:229735
34. Batuman, Olcay; Brodsky, Jeffrey L. Methods for heat shock protein
dependent cancer treatment. PCT Int. Appl. (2009), 97pp. CODEN: PIXXD2
WO 2009023846 A2 20090219 CAN 150:229672 AN 2009:198440
35. Wang, Yan; Pachter, Jonathan A.; Hailey, Judith Anne; Brams, Peter;
Williams, Denise; Srinivasan, Mohan; Feingersh, Mary Diane.
Anti-insulin-like growth factor 1 receptor therapy. PCT Int. Appl.
(2009), 129pp. CODEN: PIXXD2 WO 2009005673 A1 20090108 CAN 150:119716 AN
2009:25215
36. Janca, Michal; Dobrovolny, Petr. Preparation of bortezomib, a
boronic acid dipeptide. PCT Int. Appl. (2009), 22pp. CODEN: PIXXD2 WO
2009004350 A1 20090108 CAN 150:77955 AN 2009:20307
37. Yu, Tao; Belanger, David B.; Kerekes, Angela D.; Meng, Zhaoyang;
Tagat, Jayaram R.; Esposite, Sara J.; Mandal, Amit K.; Xiao, Yushi;
Kulkarni, Bheemashankar A.; Zhang, Yonglian; Curran, Patrick J.; Doll,
Ronald; Siddiqui, M. Arshad. Imidazopyrazines as protein kinase
inhibitors and their preparation and use in the treatment of kinase-mediated
diseases. PCT Int. Appl. (2008), 287pp. CODEN: PIXXD2 WO 2008156614 A2
20081224 CAN 150:77716 AN 2008:1536577
38. Davis, Paul J.; Mousa, Shaker A.; Hercbergs, Aleck. Nanoparticle and
polymer formulations for thyroid hormone analogs, antagonists, and
formulations. PCT Int. Appl. (2008), 236pp. CODEN: PIXXD2 WO 2008140507
A2 20081120 CAN 149:582490 AN 2008:1396803
39. Breitenkamp, Kurt; Rios-Doria, Jonathan; Breitenkamp, Rebecca; Sill,
Kevin N.; Skaff, Habib. Modification of biological targeting groups for
the treatment of cancer. PCT Int. Appl. (2008), 124pp. CODEN: PIXXD2 WO
2008134761 A2 20081106 CAN 149:534561 AN 2008:1339821
40. Kawasaki, Masashi; Mizuno, Hiroo; Sakamoto, Toshihiro; Suzuki,
Kimimasa; McKeown, Arlene E. Preparation of polymorphs, salts, and
solvates of
2-allyl-1-[6-(1-hydroxy-1-methylethyl)pyridin-2-yl]-6-[[4-(4-methylpiperazin-1-yl)phenyl]amino]-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one
as Wee1 kinase inhibitors. PCT Int. Appl. (2008), 59pp. CODEN: PIXXD2 WO
2008133866 A1 20081106 CAN 149:534237 AN 2008:1338192
41. Frenkel, Eugene P. Combination therapy for cancer comprising a
deacetylase inhibitor and a tyrosine kinase inhibitor. PCT Int. Appl.
(2008), 82 pp. CODEN: PIXXD2 WO 2008127659 A2 20081023 CAN 149:478756 AN
2008:1282336
42. Keana, John F. W.; Westberg, Paul; Curd, John G.; Lalani, Alshad L.
Mannich base N-oxide drugs for the treatment of cancer and other
proliferative diseases. PCT Int. Appl. (2008), 89pp. CODEN: PIXXD2 WO
2008115499 A1 20080925 CAN 149:394623 AN 2008:1157488
43. Clark, Michael P.; Lockwood, Mark A.; Wagner, Florence F.; Natchus,
Michael G.; Doroh, Brandon C. Preparation of substituted benzohydrazides
as chemokine receptor modulators. PCT Int. Appl. (2008), 629pp. CODEN:
PIXXD2 WO 2008112156 A1 20080918 CAN 149:378407 AN 2008:1123312
44. Clark, Michael P.; Lockwood, Mark A.; Wagner, Florence F.; Natchus,
Michael G. Substituted aromatic compounds as chemokine receptor
modulators and their preparation and use in the treatment of HIV
infection, proliferative diseases and cancer. PCT Int. Appl. (2008),
360pp. CODEN: PIXXD2 WO 2008109154 A1 20080912 CAN 149:355559 AN
2008:1106462
45. Atadja, Peter Wisdom; Shao, Wenlin; Bhalla, Kapil N. Combinations of
therapeutic agents comprising
N-hydroxy-3-[4-[[[2-(2-methyl-1H-indol-3-yl)-ethyl]-amino]methyl]phenyl]-2E-2-propenamide
for treating cancer. PCT Int. Appl. (2008), 73pp. CODEN: PIXXD2 WO
2008100985 A2 20080821 CAN 149:293683 AN 2008:1009042
46. Hoveyda, Hamid; Fraser, Graeme L.; Benakli, Kamel; Beauchemin,
Sophie; Brassard, Martin; Drutz, David; Marsault, Eric; Ouellet, Luc;
Peterson, Mark L.; Wang, Zhigang. Preparation and methods of using
macrocyclic modulators of the ghrelin receptor. U.S. Pat. Appl. Publ.
(2008), 178pp. CODEN: USXXCO US 2008194672 A1 20080814 CAN 149:288945 AN
2008:975261
47. Keegan, Mitchell; Grant, Steven. Combination therapy of cancer with
romidepsin and a proteasome inhibitor. PCT Int. Appl. (2008), 68pp.
CODEN: PIXXD2 WO 2008091620 A2 20080731 CAN 149:215945 AN 2008:916140
48. Smith, Roger; Nagarathnam, Dhanapalan. Preparation of
4-{4-[({3-tert-butyl-1-[3-(hydroxymethyl)phenyl]-1H-pyrazol-5-yl}carbamoyl)amino]-3-fluorophenoxy}-N-methylpyridine-2-carboxamide
as well as prodrugs and salts for treating cancer. PCT Int. Appl.
(2008), 84pp. CODEN: PIXXD2 WO 2008079968 A1 20080703 CAN 149:128822 AN
2008:804316
49. Mortimore, Michael; Young, Stephen Clinton; Everitt, Simon Robert
Lorrie; Knegtel, Ronald; Pinder, Joanne Louise; Rutherford, Alistair
Peter; Durrant, Steven; Brenchley, Guy; Charrier, Jean Damien;
O'Donnell, Michael. Preparation of 5-cyano-4-(pyrrolo[2,3-b]pyridin-3-yl)pyrimidines
as polo-like kinase (PLK) inhibitors. PCT Int. Appl. (2008), 191pp.
CODEN: PIXXD2 WO 2008079346 A1 20080703 CAN 149:128848 AN 2008:796822
50. Kolhe, Parag; Radhakrishnan, Vinay; Witchey-Lakshmanan, Leonore.
Methods and compositions for treating cancer and other disorders with an
anti-IGF1 receptor antibody or antigen-binding fragment thereof. PCT
Int. Appl. (2008), 114 pp. CODEN: PIXXD2 WO 2008076257 A2 20080626 CAN
149:102723 AN 2008:774251
|
Contact MedKoo:
Email:
sales@medkoo.com
(Keyword; CAS#; MedKoo code#)
|