Targeted Therapies

Formerly BioOncology Watch

www.tgt-therapies.com

 

JULY 2004

Abstract Highlights of the ASCO 40th Annual Meeting

June 5-8, 2004, New Orleans, LA

LYMPHOMA

Radioimmunotherapy (RIT) for follicular lymphoma.  Two studies investigated the effectiveness of RIT in patients with follicular lymphoma following induction chemotherapy.  DL Shipley and colleagues initiated 90Y-ibritumomab tiuxetan (Zevalin®) 5 weeks after completing 3 courses of CHOP-R therapy for previously untreated patients with stage II-IV follicular lymphoma.  Thirty-three patients were evaluable and 10 patients with a PR to CHOP-R therapy converted to a complete response (CR) after Zevalin treatment.  At the time of this report, 22 patients had completed therapy and been restaged; 19 patients (86%) were in CR and 3 patients had a PR.  The most commonly reported grade 4 toxicity was neutropenia (18%).  In a second study, B Link et al administered tositumomab and iodine I 131 tositumomab therapy (Bexxar®) to 30 previously untreated patients with follicular lymphoma within 56 days of completing 6 cycles of CVP.  Nine patients converted to a CR with Bexxar therapy, resulting in 24 patients who achieved a CR and 6 patients with a PR after completion of all planned treatments.  The median PFS had not been reached.  Grade 4 neutropenia and thrombocytopenia occurred in 33% and 32% of patients, respectively, and 1 patient developed acute myeloid leukemia.  These results show that RIT following standard first-line treatment regimens for patients with follicular lymphoma can induce high CR rates.  (Abstracts 6519 and 6520)

 

Intraventricular rituximab administration.  Previous studies in nonhuman primates led JL Rubenstein and colleagues to utilize intraventricular injections of rituximab via an Ommaya reservoir to treat 6 patients with recurrent or refractory CD20+ leptomeningeal non-Hodgkin's lymphoma (NHL).  Nine injections of rituximab 10 mg or 25 mg were planned and high ventricular levels were achieved.  Rituximab was detectable in the lumbar sac within 4 hours of administration and these treatments were well tolerated.  Mild leukoencephalopathy and paresthesias occurred in one patient.  Cytologic responses were achieved in 4 patients and 1 patient had a complete resolution of parenchymal disease.  In a second study, HS Schultz et al gave 10 - 40 mg doses of rituximab in 1 - 4 mL volumes either intrathecally (n = 2) or via an Ommaya reservoir (n = 4) to patients with intracranial lesions and/or leptomeningeal involvement due to CD20+ B-cell neoplasms.  Intraventricular administration resulted in rituximab concentrations that were several fold higher than those obtained with intravenous rituximab.  Doses of rituximab up to 35 mg injected thrice weekly were well tolerated in 5 of 6 patients.  Neurotoxicity related to rapid tumor lysis occurred in one patient.  Tumor cells were cleared from the cerebrospinal fluid and clinical remissions were achieved in 4 patients with leptomeningeal disease.  No effect on parenchymal disease was noted.  These preliminary data suggest that the intraventricular administration of rituximab is a potentially promising means of therapy for B-cell NHL patients with CNS involvement.  (Abstracts 6593 and 1521)   

 

Maintenance rituximab.  HS Hochster and others in the Eastern Cooperative Oncology Group (ECOG) performed a phase III study in which 322 patients with advanced follicular or small lymphocytic NHL received CVP chemotherapy to maximum response (6-8 cycles) and were then randomized to rituximab 375 mg/m2 i.v. weekly x 4 every 6 months for 4 cycles or observation.  The 2 study arms were well balanced for prognostic factors.  The estimates of progression-free survival (PFS) rates for 303 evaluable patients at 2 and 4 years after randomization were 74% vs. 42% and 58% vs. 34% for rituximab-treated and observation patients, respectively (p = 0.00008 [one-sided]).  The estimated 2-year survival rates were 95% for the rituximab-treated patients and 91% for the patients in the observation group.  These data demonstrate that maintenance rituximab therapy after CVP is associated with improved PFS in patients with advanced indolent NHL and have resulted in an early termination of the study.  (Abstract 6502) 

 

BEVACIZUMAB PLUS GEMCITABINE

Pancreatic cancer.  Preclinical studies suggest that anti-VEGF antibodies potentiate the activity of gemcitabine.  These findings led HL Kindler and others to study the combination of bevacizumab plus gemcitabine (BG) in previously untreated patients with advanced pancreatic cancer in a phase II trial.  Among 42 patients with evaluable data, 9 patients (21%) achieved a response and 19 patients (45%) had stable disease.  The median duration of response was 9.4 months and the median time to progression was 5.8 months.  The 6-month survival rate was 74% (median overall survival time of 9.0 months).  Plasma VEGF levels have not been found to correlate with response or survival.  The most commonly reported grade 3 and 4 toxicities have been neutropenia (33%), thrombocytopenia (7%), thrombosis (12%), and bowel perforation (5%). These encouraging results warrant further investigation.  (Abstract 4009) 

 

BEVACIZUMAB PLUS ERLOTINIB

Combined VEGF and EGFR inhibition.  Preclinical studies have indicated that combined blockade of VEGFR and EGFR pathways may enhance antitumor activity. In addition, early phase studies have shown no pharmacokinetic interaction between the anti-VEGF monoclonal antibody bevacizumab (Avastin®) and the EGFR tyrosine kinase inhibitor erlotinib (Tarceva®).  These findings led JD Hainsworth et al to test combination bevacizumab plus erlotinib in a phase II study of patients with metastatic renal cell carcinoma.  Among 40 evaluable patients, 10 (25%) patients had a partial response (PR) and 25 (62%) patients had either a minor response or stable disease.  With a median follow-up of 4.4 months, 27 patients remained on study at the time of the report and the actuarial PFS at 6 months was 71%.  The combination regimen was tolerated well by these patients.  A second phase II study conducted by M Dickler and associates evaluated the combination of bevacizumab and erlotinib in patients with relapsed and refractory metastatic breast cancer.  In the first 9 patients evaluable for response, 1 PR has been achieved and 2 patients have SD at 9 weeks of therapy.  These preliminary results indicate that combination bevacizumab plus erlotinib has activity in metastatic renal cell carcinoma and that further phase II investigation in patients with metastatic breast cancer is warranted.  (Abstracts 4502 and 2001)

 

THALIDOMIDE PLUS DEXAMETHASONE

Multiple myeloma.  SV Rajkumar and colleagues in ECOG conducted a phase III study (Study E1A00) in which newly diagnosed patients with advanced multiple myeloma were randomized to receive induction therapy with 4 months of either thalidomide 200 mg daily plus dexamethasone 40 mg on Days 1-4, 9-12, and 17-20 or dexamethasone alone.  After 4 months of treatment, patients went on to stem cell transplantation or they continued study treatment.  An analysis of 109 evaluable patients showed that the paraprotein response rate for the combination arm was 80% compared to 53% for patients treated with dexamethasone alone (p = 0.0023).  Among 192 patients evaluable for safety, a higher rate of grade 3 and 4 adverse events was observed in the combination arm (41% vs. 16%).  In addition, deep vein thrombosis occurred in 14% of patients treated with thalidomide plus dexamethasone compared to only 3% of patients given dexamethasone alone.  These findings demonstrate that treatment with the all oral combination of thalidomide plus dexamethasone results in high response rates that are comparable to those historically achieved with VAD chemotherapy.  The increased incidence of DVTs observed in the combination arm suggest that studies utilizing prophylactic anticoagulation in conjunction with thalidomide plus dexamethasone therapy for multiple myeloma patients are warranted.  (Abstract 6508)

 

PACLITAXEL PLUS TRASTUZUMAB

Breast cancer.  AD Seidman and associates in the Cancer and Leukemia Group B (CALGB) performed a phase III study in which patients with metastatic breast cancer who had received 0-1 prior chemotherapy regimens were randomized to either weekly or every third-week paclitaxel treatments.  After the accrual of 171 patients, when trastuzumab became a standard therapy for patients with HER2-positve breast cancer, patients with HER2-positve disease received trastuzumab and patients with HER2 normal disease were randomized for trastuzumab.  A total of 577 patients were treated.  Weekly paclitaxel was superior to every third-week paclitaxel with respect to response rate (p = 0.017 and time to progression (p = 0.0008).  A trend toward an increase in survival was also seen in the weekly paclitaxel group (p = 0.17).  Trastuzumab was not found to increase efficacy in the normal HER2 group.  Weekly paclitaxel was associated with greater neurologic toxicity, but less grade 3 or 4 granulocytopenia.  Five patients (0.8%) experienced significant cardiac dysfunction.  This study demonstrated that weekly paclitaxel is more efficacious than every third-week paclitaxel for the treatment of patients with metastatic breast cancer.  In addition, trastuzumab treatment of patients with normal HER2 metastatic breast cancer was not found to increase clinical benefit.  (Abstract 512)     

 

Bcl-2 ANTISENSE

Oblimersen sodium treatment of advanced melanoma.  Resistance of malignant melanoma to chemotherapy has been linked to overexpression of the anti-apoptotic protein, Bcl-2.  Oblimersen sodium (Genasense) downregulates Bcl-2 and may enhance apoptosis when added to chemotherapy.  In addition, previous studies showed that oblimersen sodium has activity against melanoma.  Thus, MJ Millward and coworkers conducted a phase III study in which patients with stage 4 or unresectable stage 3 melanoma were randomized to receive DTIC (1,000 mg/m2 i.v. every 3 weeks) plus oblimersen sodium (7 mg/kg/day for 5 days prior to DTIC by continuous i.v. infusion) or DTIC alone.  A higher response rate (11.7% vs. 6.8%; p = 0.019) and a longer time to progression (74 vs. 49 days; p = 0.0003) was observed in the patients treated with combination therapy.  A trend toward increased overall survival was also noted for the oblimersen sodium-treated patients (median survival of 9.1 vs. 7.9 months; p = 0.18).  Hematologic toxicity and acute phase reaction adverse events occurred more frequently in the combination therapy group.  These data suggest that oblimersen sodium may enhance the effect of DTIC against melanoma.  (Abstract 7505)

 

ERLOTINIB

Non-small-cell lung cancer (NSCLC).  In phase II studies erlotinib (Tarceva®) has demonstrated single-agent activity in patients with NSCLC.  FA Shepherd and colleagues from the National Cancer Institute of Canada Clinical Trials Group now report the results of a double-blind phase III study in which stage IV or IIIB NSCLC patients were randomized in a 2:1 ratio to receive either erlotinib or placebo after failing first or second line therapy (N = 731).  The response rate to erlotinib was 8.9% and the median duration of response was 34.2 weeks.  Improved overall and progression-free survival times were observed in the erlotinib-treated patients compared to those who received placebo (6.7 vs. 4.7 months; p = 0.001 and 2.23 vs. 1.84 months; p < 0.001, respectively).  The times to the development of tumor-related symptoms were also longer in the erlotinib group. These results demonstrate that erlotinib therapy prolongs survival compared to placebo treatments in previously treated patients with advanced NSCLC.  (Abstract 7022)  

 

CETUXIMAB

Combined with chemotherapy in colorectal cancer (CRC).  The findings of 2 trials investigating the combination of cetuximab (Erbitux®) with standard chemotherapy regimens in patients with CRC were reported.  P Rougier and colleagues combined weekly i.v. cetuximab at doses of either 400 or 250 mg/m2 with FOLFIRI (irinotecan, 5FU, folinic acid) in a phase II study of previously untreated patients with metastatic EGFR+ CRC.  Dose-limiting toxicity (DLT) was not experienced in the lower dose cetuximab group while 3 patients in the high-dose group had DLTs consisting of diarrhea, an allergic reaction, and neutropenia.  Among 22 evaluable patients, 10 patients (46%) achieved a PR and 9 patients (41%) had stable disease.  The median time to progression was 10.9 months.  These results indicate that the combination of cetuximab with chemotherapy regimens is feasible in patients with metastatic CRC.  S Badarinath et al reported a preliminary safety analysis of a phase III study in which patients with metastatic EGFR+ CRC were randomized to receive second-line therapy with cetuximab (400 mg/m2 initial dose followed by 250 mg/m2 weekly) plus FOLFOX4 (5FU, leucovorin, oxaliplatin) or FOLFOX4 alone.  This analysis of 40 patients indicated that cetuximab did not increase the toxicity associated with FOLFOX4 and that the authors were continuing to accrue the target sample size of 1100 patients.  (Abstracts 3513 and 3531) 

 

Squamous cell carcinoma (SCC) of head and neck.  JA Bonner et al conducted a phase III study in which patients with locoregionally advanced SCC of the oropharynx, hypopharynx, or larynx were randomized to receive weekly cetuximab plus radiation or radiation alone (N = 424).  The median survival for patients given cetuximab plus radiation was 54 months compared to 28 months for patients who received radiation alone (P = 0.02).  Toxicity was similar between the treatment groups except that an increased incidence of grade 3 and 4 skin reactions occurred in the cetuximab-treated patients (34% vs. 18%; p = 0.0003).  These data show that the addition of cetuximab to radiation improved survival in patients with locally advanced SCC of the head and neck and suggest that cetuximab should be studied in other tumors associated with EGFR overexpression.  (Abstract 5507) 

 

SIGNAL TRANSDUCTION INHIBITION

Renal cell carcinoma (RCC).  RJ Motzer et al investigated the use of an orally administered tyrosine kinase inhibitor, SUO11248, as treatment for 63 patients with metastatic RCC.  SUO11248 was given at a dose of 50 mg once daily for 4 weeks every 6 weeks.  The early best-response data revealed that 15 patients (24%) achieved a PR, 29 patients (46%) had stable disease, and 19 patients (30%) developed disease progression.  With a median follow-up of 6+ months, 32 patients remained on study treatment.  SUO11248 was tolerated with acceptable toxicity.  The most commonly reported grade 3 or 4 adverse events were lymphopenia (30%) and elevated lipase levels (21%).  Eight percent of patients had increased levels of amylase without pancreatitis and 2 patients developed a decrease in left ventricular ejection fraction.  In a second investigation, MJ Ratain et al. studied Bay 43-9006 (BAY), a novel agent that inhibits tumor proliferation and angiogenesis through blockade of the Raf/MEK/ERK pathway at the level of Raf kinase and the receptor kinases VEGFR-2 and PDGF-b.  The authors enrolled 397 patients with advanced solid tumors in a placebo-controlled, randomized discontinuation phase II trial.  Tumor regression was noted in multiple tumor types.  Among 63 evaluable patients with RCC, 25 patients responded to treatment and 18 patients had stable disease.  The most common toxicities were rash, hand-foot syndrome, fatigue, diarrhea, anorexia, and hypertension.  These studies demonstrate early evidence of antitumor activity for these novel agents.  (Abstracts 4500 and 4501)

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