Bortezomib Millennium Pharmaceuticals

IDrugs

Volumn 5, Issue 8, 2002, Pages 828-834

  Dou, Q Ping ^a   Goldfarb, Ronald H ^b  

^a H LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE   (United States)

^b UNIVERSITY OF NORTH TEXAS HEALTH SCIENCE CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; ANTINEOPLASTIC HORMONE AGONISTS AND ANTAGONISTS; BORTEZOMIB; CYTOTOXIC AGENT; DACLIZUMAB; DEXAMETHASONE; DOCETAXEL; DOXORUBICIN; FLUOROURACIL; FOLINATE CALCIUM; GEMCITABINE; IRINOTECAN; MELPHALAN; MITOXANTRONE; NSC 681239; PROTEINASE INHIBITOR; PS 273; PS 293; PS 304; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; CANCER; CANCER INHIBITION; CLINICAL TRIAL; DIARRHEA; DOSE RESPONSE; DRUG BINDING; DRUG BLOOD LEVEL; DRUG CYTOTOXICITY; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG INDICATION; DRUG METABOLISM; DRUG POTENTIATION; DRUG SAFETY; DRUG SYNTHESIS; DRUG TOXICITY; ENZYME INHIBITION; FATIGUE; HUMAN; NAUSEA; NONHUMAN; PERIPHERAL NEUROPATHY; PROSTATE CANCER; REVIEW; STRUCTURE ACTIVITY RELATION; THROMBOCYTOPENIA;

EID: 0346692671     PISSN: 13697056     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (47)

1. 199269 Inhibition of proteasome-dependant activation of NFκB: A novel strategy for the development of anti-inflammatory agents. Stein RL Anti-infamm Drug Disc Summit 1996 February 12
2. 279542 Potent and selective inhibitors of the proteasome: Dipeptidyl boronic acids. Adams J, Behnke M, Chen S, Cruickshank AA, Dick LR, Greneir L, Klunder JM, Ma YT, Plamondon L, Stein RL Bioorg Med Chem Lett 1998 8 4 333-338 Synthesis and SAR of bortezomib.
3. 301435 ProScript initiates phase I trial for a new class of cancer therapeutics. ProScript Inc Press Release 1998 October 14
4. 310946 ProScript and NCI collaborate on anticancer therapeutic. ProScript Inc Press Release 1999 January 07
5. 312219 New rat study delineates RA benefits of ProScript small molecule. Bioworld Week 1998 6 51 3
6. 335483 Proteasome inhibitors: A novel class of potent and effective antitumor agents. Adams J, Palombella VJ, Sausville EA, Johnson J, Destree A, Lazarus DD, Maas J, Pien CS, Prakash S, Elliott PJ Cancer Res 1999 50 11 2615-2622 Report on SAR, apoptosis-inducing activity, antitumor activity and pharmacodynamics of bortezomib.
7. 362119 Proteasone inhibitor PS-341 effective as an anti-angiogenic agent in the treatment of human pancreatic carcinoma via the inhibition of NFκB and subsequent inhibition of vascular endothelial growth factor production. Harbison MT, Bruns CJ, Bold RJ, Elliot PJ, Adams J, Abruzzese JL, McConkey DJ Proc Annu Meet Am Assoc Cancer Res 2000 41 April 1-5 Abs 453
8. 382079 Protease inhibitor-induced apoptosis: Accumulation of wt p53, p21WAF1/CIP1, and induction of apoptosis are independent markers of proteasome inhibition. An WG, Hwang SG, Trepel JB, Blagosklonny MV Leukemia 2000 14 7 1276-1283 Demonstration of apoptosis-inducing activity of bortezomib in human leukemic cell lines.
9. 392555 Millennium Pharmaceuticals Inc - Product pipeline. Millennium Pharmaceuticals Inc Company World Wide Web Site 2000 December 07
10. 393823 PS-341 is active in multiple myeloma: Preliminary report of a phase I trial of the proteasome inhibitor PS-341 in patients with hematologic malignancies. Stinchcombe TE, Mitchell BS, Depcik-Smith N, Adams J, Elliott P, Shea TC, Orlowski RZ Blood 2000 96 11 Suppl 1 Abs 2219
11. 396071 Proteasone inhibition measurements: Clinical application. Lightcap ES, McCormack TA, Pien CS, Chau V, Adams J, Elliott PJ Clin Chem 2000 46 5 673-683 Report on fluorogenic kinetic assays for the proteasome activities optimized for both whole blood and blood cells.
12. 400636 Millennium initiates phase II clinical trials of LDP-341 in multiple myeloma: Lead development compound in the oncology franchise area advances in clinic. Millennium Pharmaceuticals Inc Press Release 2001 March 01
13. 403615 American Association for Cancer Research 92nd Annual Meeting (Part VII), New Orleans, LA, USA. Jones E IDDB Meeting Report 2001 March 24-28 Report of studies that demonstrate that bortezomib overcomes Bcl-2-mediated inhibition of apoptosis.
14. 404054 Enhancement in cytotoxicity of Taxotere with proteasome inhibitor (PS-341) in human ovarian cancer. Ng B, Elliot P, Adams J, Muggia F, Liebes L Proc Annu Meet Am Assoc Cancer Res 2001 42 March 24-28 Abs 252
15. 409901 Clinical development of a proteasome inhibitor, PS-341, for the treatment of cancer. Nix D, Pien C, Newman R, Madden T, Felix E, Adams J, Elliott P Proc Am Soc Clin Oncol 2001 20 Pt 1 Abs 339 Report on regimen-independent, dose-dependent and reversible inhibition of 20S proteasome activity by brotezomib in a phase I clinical trial.
16. 409902 Phase I study of intravenous (IV) proteasome inhibitor PS-341 in patients (Pts) with advanced malignancies. Papandreou C, Daliani D, Millikan RE, Tu S, Pagliaro L, Adams J, Elliott P, Nix D, Dieringer P, Thall P, Logothesis CJ Proc Am Soc Clin Oncol 2001 20 Pt 1 Abs 340
17. 410434 Dose dependent inhibition of 20S proteasome results in serum II6 and PSA decline in patients (PTS) with androgen-independent prostate cancer (AI PCa) treated with proteasome inhibitor PS-341. Logothesis CJ, Yang H, Daliani D, Millikans RE, Tu S, Pagliaro L, Adams J, Elliott P, Nix D, Kieringer P, Papandreou CN Proc Am Soc Clin Oncol 2001 20 Pt 1 Abs 740
18. 412700 Millennium initiates combination trials of LDP-341 with gemcitabine and irinotecan. Millennium Pharmaceuticals Inc Press Release 2001 June 14
19. 412848 Millennium initiates phase II clinical trials of LDP-341 in chronic lymphocytic leukemia - Proteasome inhibitor advances in clinical development for hematologic indications. Millennium Pharmaceuticals Inc Press Release 2001 June 15
20. 420411 American Chemical Society - 222nd National Meeting - Overnight Report (Part IV), Chicago, IL, USA. Swords B IDDB Meeting Report 2001 August 26-30
21. 424437 Millennium completes enrollment of a phase II human clinical trial for LDP-341 in multiple myeloma. Millennium Pharmaceuticals Inc Press Release 2001 October 04
22. 427632 The proteasome inhibitor PS-341 inhibits growth, induces apoptosis, and overcomes drug resistance in human multiple myeloma cells. Hideshima T, Richardson P, Chauhan D, Palombella VJ, Elliott PJ, Adams J, Anderson KC Cancer Res 2001 61 7 3071-3076
23. 427722 Pharmacological proteasome inhibitors and their therapeutic potential. Dou QP, Nam S Exp Opin Ther Pat 2000 10 8 1263-1272 A comprehensive review on proteasome inhibitors.
24. 427857 Millennium researchers announce initial findings of phase I trial of proteasome inhibitor for multiple myeloma. Millennium Pharmaceuticals Inc Press Release 2001 November 02 Additive effect of bortezomib and chemotherapy in mice harboring human colon cancer.
25. 429576 Molecular targets and cancer therapeutics - AACR-NCI-EORTC International Conference (Part I), discovery, biology, and clinical applications, Miami Beach, FL, USA. D'Incalci M, Damia G IDDB Meeting Report 2001 October 29-November 02 Report demonstrating antitumor activity of bortezomib in various phase I clinical trials of prostate cancer, acute myeloid leukemia and MM.
26. 429923 The proteasome inhibitor PS-341 inhibits metastases in a Lewis lung carcinoma model by cytotoxicity and antiangiogenesis. Lin J, Pien C, Pink M, Adams J, Elliott P AACR NCI EORTC Mol Targets Cancer Ther 2001 October 29-November 02 Abs 67A
27. 432453 NFκB as a therapeutic target in multiple myeloma (MM). Hideshima T, Chauhan D, Castro A, Hayashi T, Mitsiades C, Mitsiades N, Akiyama M, Richardson PG, Schlossman RL, Adams J, Anderson KC Blood 2001 98 11 Suppl 1 Abs 1581 Inhibition of IκBα degradation and NFκB activation by bortezomib in MM.
28. 432519 Anti-tumor activity of the proteasome inhibitor PS-341 in mantle cell lymphoma B cells. Pham L, Tamayo A, Lo P, Yoshimura L, Ford RJ Blood 2001 98 11 Suppl 1 Abs 1945
29. 432540 Proteasome inhibitor PS-341 markedly enhances sensitivity of multiple myeloma cells to chemotherapeutic agents and overcomes chemo-resistance through inhibition of the NFκB pathway. Ma MH, Parker KM, Manyak S, Altamirano CV, Wu ZQ, Borad MJ, Roussos E, Neeser J, Mikail A, Frantzen M, Adams J et al. Blood 2001 98 11 Suppl 1 Abs 1978
30. 432996 New phase II data on Millennium's proteasome inhibitor holds promise for patients with refractry multiple myeloma - Investigational compound shown to stop the progression of disease in patients whose disease has progressed on multiple prior therapies. Millennium Pharmaceuticals Inc Press Release 2001 December 10
31. 435062 Millennium initiates combination oncology trials of MLN341 with Taxotere - Furthers aggressive clinical development program of investigational compound in solid tumors in conjunction with chemotherapy agent. Millennium Pharmaceuticals Inc Press Release January 07
32. 441325 The proteasome: A new target for novel drug therapies. Elliot PJ, Ross JS Am J Clin Pathol 2001 116 5 637-646 A comprehensive review on proteasome inhibitors.
33. 441326 Proteasome inhibition in cancer: Development of PS-341. Adams J Semin Oncol 2001 28 6 613-619 A comprenhensive review on proteasome inhibitors.
34. 441329 Development of the proteasome inhibitor PS-341. Adams J Oncologists 2002 7 1 9-16 A comprensive review on proteasome inhibitors.
35. 441816 CEP-1612, a dipeptidyl proteasome inhibitor, induces p21WAF1 and p27KIP1 expression and apoptosis and inhibits the growth of the human lung adenocarcinoma A-549 in nude mice. Sun J, Nam S, Lee CS, Li B, Coppola D, Hamilton AD, Dou QP, Sebti SM Cancer Research 2001 61 4 1280-1284
36. 441818 Novel dipeptidyl proteasome inhibitors overcome Bcl-2 protective function and selectively accumulate the cyclin-dependent kinase inhibitor p27 and induce apoptosis in transformed, but not normal, human fibroblasts. An B, Goldfarb RH, Siman R, Dou QP Cell Death Differentiation 1998 5:1065-1075 Studies demonstrating that the dipeptidyl aldehyde proteasome inhibitor CEP-1612 overcome Bcl-2-mediated protection and selectively induces apoptosis in tumor and transformed cells.
37. 444408 NFκB: Bench to Bedside - Keystone Symposium, Keystone, CO, USA Amit S, Ben Neriah Y IDDB Meeting Report 2002 25 February-3 March
38. 449061 Proteasome inhibitor PS-341, a potential therapeutic agent for adult T-cell leukemia. Tan C, Wladmann TA Cancer Res 2002 62 4 1083-1086 Report on inhibition of IκBα degradation and NFκ activation, as well as enhancement of other therapeutic drug effects by bortezomib in an adult T-cell leukemia murine model.
39. 451822 A phase I and pharmacodynamic study of the proteasome inhibitor PS-341 in combination with doxorubicin. Thomas JP, Arzoomanian R, Alberti D, Geiger P, Marnocha R, Tutsch K, Dresen A, Volkman J, Binger K, Kolb M, Feierabend C et al. Proc Am Soc Clin Oncol 2002 21 1 Abs 368
40. 451824 Phase I dose-escalation study of the proteasome inhibitor, PS-341, plus irinoteca in patients with advanced solid tumors. Clark JW, Ryan D, Dees C, Eder JP, Winkelmann J, Lynch T, Supko J, Appleman LJ, Fidias P, O'Nell B, Orlowski RZ et al. Proc am Soc Clin Oncol 2002 21 1 Abs 369
41. 451828 Phase I study of PS-341 in combination with 5-FU/LV in solid tumors. Iqbal S, Lenz HJ, Groshen S, Wei Y, Gandara DR, Lara PN, Gumerlock P, Doroshow JH, Twardowski P, Synold T Proc Am Soc Clin Oncol 2002 21 1 Abs 370
42. 451862 Pharmacokinetic and pharmacodynamic phase I study of PS-341 and gemcitabine in patients with advanced solid tumors. Ryan DP, Eder JP, Winkelmann J, Lynch T, Supko J, Appleman LJ, Fidias P, Enzinger P, Zhu A, Kinchla N, Esseltine D et al. Proc Am Soc Clin Oncol 2002 21 1 Abs 379
43. 451738 American Society of Clinical Oncology - 38th Annual Meeting (Part V) - OVERNIGHT REPORT, Orlando, FL, USA. Evans L Meeting Report 2002 May 18-21
44. 452675 Mechanisms of enhanced cytotoxicity from Docetaxel (R) PS-341 combination in non-small cell lung carcinoma (NSCLC). Gumerlock PH, Kawaguchi T, Moison LP, Lau AH, Mack PC, Lara PN, Gandara DR Proc Am Soc Clin Oncol 2002 21 1 Abs 1214
45. 453557 FDA grants Millennium's MLN341 and MLN518 fast track status. Millennium Pharmaceuticals Inc Press Release 2002 June 05
46. 454446 Millennium initiates pivotal phase III clinical trial comparing VELCADE(TM) (bortezomib) for injection with high-dose dexamethasone in patients with multiple myeloma. Millennium Pharmaceuticas Inc Press Release 2002 June 11
47. 456917 Proteasome inhibitors: From research tools to drug candidates. Kisselev AF, Goldberg AL Chem Biol 2001 8 8 739-758 A comprenhensive review on various proteasome inhibitors.