Interleukin 21 (IL-21)
IL-21 has demonstrated anti-tumor activity in Phase 2 clinical trials
Interleukin-21 (IL-21) is a cytokine with potential use in the treatment of cancer. ZymoGenetics is testing recombinant IL-21 in a Phase 2 clinical trial in collaboration with the National Cancer Institute of Canada in patients with metastatic melanoma. Previously, the company demonstrated anti-tumor activity in a Phase 2 clinical trial in combination with Nexavar® in patients with metastatic renal cell carcinoma. In October 2005, the FDA granted IL-21 orphan drug status for the treatment of melanoma patients with advanced or aggressive disease. ZymoGenetics has worldwide development and commercialization rights to IL-21 after securing ex-North American rights from Novo Nordisk A/S in January 2009.
Background
Endogenous IL-21 is a potent regulator of key classes of immune cells, including cytotoxic T lymphocyte cells and natural killer cells. These cell types play critical roles in eliminating malignant and virally infected cells from the body. IL-21 also is important in boosting antibody response, another weapon in the body's fight against cancer. The combined biologic actions of IL-21 suggest that it may be an effective immunotherapy in the treatment of cancer, either alone or in combination with other anti-cancer drugs. Based on preclinical and early clinical trial data, IL-21 could potentially be better tolerated and more efficacious than other currently marketed immunotherapies for cancer, such as interleukin-2 (IL-2) and interferon-alpha.
Clinical Trials
ZymoGenetics is pursuing metastatic melanoma as the initial indication for IL-21. A Phase 1 monotherapy trial of IL-21 in patients with metastatic renal cell carcinoma and metastatic melanoma demonstrated a favorable safety profile for use in an outpatient setting and evidence of anti-tumor activity in both indications. Based on these Phase 1 results, ZymoGenetics is continuing development of IL-21 in metastatic melanoma as a single agent in collaboration with the National Cancer Institute of Canada. In August 2009, patient enrollment was completed in an open-label, multi-center Phase 2 study of recombinant IL-21 for first line treatment of patients with advanced metastatic melanoma. Interim results from this trial were presented in 2009, and final results are expected to be available in 2010.
Market Opportunity
Metastatic Melanoma
Metastatic melanoma now ranks as one of the most common cancers in the United States and Europe. In 2007, there were approximately 115,000 new cases of metastatic melanoma in the United States, Europe and Japan. Over the next ten years the number of newly diagnosed cases of metastatic melanoma is expected to increase by 32% in these markets.
Scientific Publications
Phase 2
- ASCO 2010 Presentation: IL-21 Phase 2 Metastatic Melanoma Results (PDF)
- ASCO 2010 Abstract: IL-21 Phase 2 Metastatic Melanoma Results (PDF)
- ASCO 2009: IL-21 ASCO Renal Cell Cancer Results from a Phase 2 Clinical Trial (PDF)
- 7th World Congress on Melanoma, Vienna, Austria, May 2009: IL-21 Metastatic Melanoma Phase 2 Interim Results (PDF)
- Abstract for the 7th World Congress on Melanoma, Vienna, Austria, May 2009: IL-21 Metastatic Melanoma Phase 2 Interim Results (PDF)
- EORTC-NCI-AACR 2008: Recombinant IL-21 in Combination with Sorafenib as Second- or Third-Line Therapy for Metastatic Renal Cell Carcinoma (mRCC): Interim Results from a Phase 2 Study (PDF)
Phase 1
- Phase I study of recombinant interleukin-21 in patients with metastatic melanoma and renal cell carcinoma: J Clin Oncol 2008;26(12):2034-39
- iSBTC 2008: Recombinant Interleukin-21 Plus Sorafenib for Metastatic Renal Cell Carcinoma (mRCC): A Phase 1 Dose Escalation Study (PDF)
- ASCO 2008: Efficacy and Safety of Recombinant Interleukin-21 (rIL-21) and Rituximab in Relapsed/Refractory Indolent Lymphoma (PDF)
- AACR-NCI-EORTC 2007: Recombinant IL-21 (rIL-21) in Combination with Sorafenib: Preliminary Results from a Phase I/II Study in Patients with Metastatic Renal Cell Cancer (RCC) (PDF)
- ASH 2007: Recombinant Interleukin-21 (rIL-21) Plus Rituximab Clinical Activity in a Phase 1, Dose-Finding Trial in Relapsed Indolent B Cell Lymphoma (PDF)
- ASCO 2006: Recombinant Interleukin-21 (IL-21) Tolerability and antitumor activity following two 5-day cycles in patients with stage IV melanoma (MM) or renal cell carcinoma (RCC) (PDF)
- ASCO 2005: Preliminary Tolerability and Anti-tumor Activity of Intravenous Recombinant Human Interleukin-21 (IL-21) in Patients With Metastatic Melanoma and Metastatic Renal Cell Carcinoma (PDF)
Preclinical
- Immune activation in advanced cancer patients treated with recombinant IL-21: multianalyte profiling of serum proteins: Cancer Immunol Immunother 2009;58(6):843-54. Epub 2008 Oct 17
- Interleukin-21 augments the efficacy of T-cell therapy by eliciting concurrent cellular and humoral responses: Cancer Res 2008;68(11):4431-41
- Interleukin 21 enhances antibody-mediated tumor rejection: Cancer Res 2008;68(8):3019-25
- IL-21 induces in vivo immune activation of NK cells and CD8+ T cells in patients with metastatic melanoma and renal cell carcinoma: Cancer Immunol Immunother 2008; 57(10):1439-49
- Interleukin-21 signaling: functions in cancer and autoimmunity: Clin Cancer Res, 2007, 13(23): 6926-32
- Combined IL-21 and low-dose IL-2 therapy induces anti-tumor immunity and long-term curative effects in a murine melanoma tumor model: J Transl Med, 2006, 4: 24
- IL-21 enhances tumor-specific CTL induction by anti-DR5 antibody therapy: J Immunol, 2006, 176(10): 6347-55
- IL-21 enhances tumor rejection through a NKG2D-dependent mechanism: J Immunol, 2005, 175(4): 2167-73
- IL-21 enhances and sustains CD8(+) T cell responses to achieve durable tumor immunity: comparative evaluation of IL-2, IL-15 and IL-21: J Immunol, 2004, 173(2): 900-9
- Interleukin-21 is a T-helper cytokine that regulates humoral immunity and cell-mediated anti-tumour responses: Immunology, 2004, 112(2): 177-82
- Cutting edge: IL-21 is a switch factor for the production of IgG1 and IgG3 by human B cells: J Immunol, 2004, 172(9): 5154-7
- Interleukin-21 inhibits dendritic cell activation and maturation: Blood, 2003, 102(12): 4090-8
- IL-21 in synergy with IL-15 or IL-18 enhances IFN-gamma production in human NK and T cells: J Immunol, 2003, 170(11): 5464-9
- Human IL-21 and IL-4 bind to partially overlapping epitopes of common gamma-chain: Biochem Biophys Res Commun, 2003, 300(2): 291-6
- Interleukin-21 prevents antigen-induced IgE production by inhibiting germline C{epsilon} transcription of IL-4-stimulated B cells: Blood, 2002, 100(13): 4565-73
- Interleukin-21 and the IL-21 receptor: novel effectors of NK and T cell responses: J Leukoc Biol, 2002, 72(5): 856-63
- IL-21 up-regulates the expression of genes associated with innate immunity and Th1 response: J Immunol, 2002, 169(7): 3600-5
- Cutting edge: the common gamma-chain is an indispensable subunit of the IL-21 receptor complex: J Immunol, 2001, 167(1): 1-5
- Interleukin 21 and its receptor are involved in NK cell expansion and regulation of lymphocyte function: Nature, 2000, 408(6808): 57-63
Press Releases
- Jun 5, 2010 ZymoGenetics Reports Positive IL-21 Phase 2 Results in Metastatic Melanoma
- May 20, 2010 ZymoGenetics Announces Upcoming Presentation of Positive IL-21 Phase 2 Results in Metastatic Melanoma at ASCO Meeting
- May 31, 2009 ZymoGenetics Reports Encouraging Phase 2 Results in Renal Cell Cancer for IL-21 with Nexavar
- May 14, 2009 Final Phase 2 Reults for IL-21 in Renal Cell Cancer Show Tolerability and Enhanced Efficacy of Nexavar Combination
- May 13, 2009 ZymoGenetics Reports Encouraging Preliminary Results from Phase 2 Study of IL-21 in Metastatic Melanoma Conducted by NCIC
- Jan 28, 2009 ZymoGenetics Secures Worldwide Rights to IL-21
- Nov 10, 2008 ZymoGenetics Presents Interim IL-21 Phase 2 Results in Renal Cell Cancer
- May 15, 2008 ZymoGenetics Announces Publication of Five IL-21 ASCO Abstracts
- Jan 8, 2008 ZymoGenetics Begins Phase 2 Trial in Renal Cell Cancer Evaluating IL-21 Combined with Nexavar(R)
- Dec 18, 2007 ZymoGenetics Begins Phase 2 Clinical Trial of IL-21 in Melanoma
- Dec 10, 2007 ZymoGenetics Presents Positive Interim Phase 1 Results for IL-21 in Combination with Rituxan(R) in B Cell Lymphoma
- Oct 23, 2007 ZymoGenetics Reports Positive Phase 1 Results for IL-21 With Nexavar(R)
- Oct 17, 2006 ZymoGenetics Begins Phase 1/2 Clinical Trial With IL-21 and Nexavar in Patients With Renal Cell Cancer
- Jul 12, 2006 ZymoGenetics Begins Phase 1 Trial With IL-21 and Rituxan(R) in Patients With Non-Hodgkin's Lymphoma
- Jun 5, 2006 ZymoGenetics Reports Encouraging IL-21 Phase 1b Results in Metastatic Melanoma and Renal Cell Cancer Presented at ASCO Meeting
- Nov 14, 2005 ZymoGenetics Presents IL-21 Clinical Study Results at International Society for Biological Therapy of Cancer Conference
- Oct 5, 2005 FDA Grants Orphan Drug Designation to ZymoGenetics' IL-21 for Treatment of Melanoma
- May 16, 2005 ZymoGenetics Interleukin 21 Phase 1 Data Presented at ASCO Annual Cancer Meeting; Interim Results Show Potential to Treat Metastatic Melanoma and Renal Cell Carcinoma
- May 9, 2005 ZymoGenetics to Present at ASCO Annual Meeting; Three IL-21 Presentations to Be Given at Cancer Meeting
- Jun 7, 2004 ZymoGenetics Presents Preclinical Interleukin 21/Antibody-Based Cancer Therapy Data at ASCO; Preclinical Studies Suggest Clinical Utility in Combination Cancer Therapy
- Apr 5, 2004 ZymoGenetics to Begin Clinical Study with Interleukin 21; FDA gives go ahead to proceed with Phase 1 cancer study
- Jul 14, 2003 ZymoGenetics Demonstrates Anti-tumor Activity with Interleukin-21
- Jan 9, 2003 ZymoGenetics and Novo Nordisk Enter into Preclinical Development Alliance for Interleukin 21; Companies to Share Costs and Preclinical Data Leading up to IND Filing
- Oct 9, 2002 ZymoGenetics Adds Interleukin-21 (IL-21) to Its Product Development Pipeline
- Nov 2, 2000 ZymoGenetics Researchers Identify Novel Interleukin that Plays Key Role in Immune System Regulation


