BioOncology Watch

Timely Information for Practicing Physicians

 

july 2003

highlights of the 39th ASCO Annual Meeting May 31 to June 3, 2003, Chicago, IL

HER2-TARGETED THERAPY

Cardiac safety of trastuzumab (T).  M. Marty and colleagues pooled data from 4 clinical trials in which left ventricular ejection fraction (LVEF) was monitored in 259 patients treated with T.  Five cases of symptomatic cardiac failure were reported and 15 LVEF events were identified.  Prior anthracycline use was associated with a 5-fold higher risk of an event in patients treated with T.  These findings support conclusions of prior retrospective analyses of T-related cardiotoxicity and indicate that the overall risk-benefit ratio for treatment of HER2-positive metastatic breast cancer (MBC) remains favorable.  A second abstract by A.C. Wolff et al. reported interim results from a multicenter ECOG trial (E3198) that is evaluating the cardiac safety of patients with HER2-positive MBC treated with T in combination with pegylated liposomal doxorubicin and docetaxel compared to that of patients with HER2-negative MBC treated with doxorubicin and docetaxel alone.  Data from 22 evaluable T plus doxorubicin and docetaxel-treated patients showed an average drop of 3.6% and no > grade 2 cardiac events after 4 cycles.  Accrual to this study remains ongoing.  A third study by H. Joensuu and the Finnish Breast Cancer Group demonstrated that T in combination with vinorelbine or docetaxel adjuvant therapy for early BC is not associated with short-term cardiotoxicity.  High-risk BC patients (N = 606) were randomized to receive adjuvant vinorelbine (8 weekly cycles) or docetaxel (3 cycles).  HER2-positive patients were also randomized to receive or not to receive T (9 weekly infusions) in combination with vinorelbine or docetaxel.  Following these treatments, all patients were given 3 weekly cycles of CEF60 and ER+ patients also received tamoxifen for 5 years.  The mean LVEF at baseline, during the last chemotherapy cycle, and 6 months after completing chemotherapy were 65%, 64%, and 64%, respectively, for T-treated patients compared to 67%, 64%, and 64%, respectively, for patients treated with vinorelbine or docetaxel alone.  These 3 studies suggest a favorable risk-benefit ratio for T treatment of HER2-positive BC. (Abstracts 72, 70, and 74)

 

Phase I study of pertuzumab.  Pertuzumab is a humanized HER2 antibody that binds to a different epitope than trastuzumab and inhibits intracellular signaling through MAP kinase and PI3 kinase pathways.  Twenty-one patients with advanced solid tumors received pertuzumab intravenously every 3 weeks at one of the following doses: 0.5 (n = 3); 2 (n = 3); 5 (n = 4); 10 (n = 3); or 15 mg/kg (n = 8).  Only 2 grade 3 or 4 adverse events were assessed to be possibly pertuzumab-related: a gastrointestinal bleed and left ventricular failure following a myocardial infarction.  Despite monitoring with 2-D echocardiograms and serologic markers, no other evidence of cardiac dysfunction was detected.  Three (14%) patients achieved partial responses and 8 (38%) patients had stable disease that persisted for a median of 13.7 weeks (range, 6.1 to 24.4 weeks).  These preliminary data show that pertuzumab is well tolerated at doses up to 15 mg/kg and is potentially active clinically.  (Abstract 771)

 

INHIBITORS OF EGFR

GW572016.  GW572016 is a novel small molecule inhibitor of EGFR and ErbB2. N.  Spector and associates reported the findings of a phase I study in which patients with metastatic carcinomas that overexpress EGFR or ErbB2 were randomized to receive one of 5 doses of GW572016 (500, 650, 900, 1200, or 1600 mg) administered orally once daily.  Twenty-eight patients were accrued and of 10 evaluable patients, 2 trastuzumab-resistant BC patients had objective responses.  Toxicities were primarily gastrointestinal (diarrhea) and dermatologic (transient rashes) and were not dose dependent.  In addition, M. S. Berger et al. treated patients with trastuzumab-refractory MBC with GW572016 1250 mg daily in a phase II study.  As of December 2002, 3 patients had been accrued and no cardiac toxicity had been reported.  Enrollment is ongoing.  (Abstracts 772 and 981)

 

FLT3 INHIBITORS IN ACUTE MYELOID LEUKEMIA (AML)

Phase II studies of 2 novel agents.  CEP-701, an indolocarbazole derivative that inhibits FLT3 with an IC50 in the range of 1-2 nM in vitro, has been shown to cause cell death and prolong survival in an AML mouse model.  Early results of a phase II study of CEP-701 treatment in patients with refractory or relapsing AML expressing FLT3-activating mutations were presented by B.D. Smith and colleagues.  The CEP-701 dose was increased from 40 to 60 mg BID after ex vivo analysis showed incomplete inhibition of FLT3 autophosphorylation in the first 3 patients.  Short-lived clinical responses (decrease of peripheral blood [PB] blasts to <5% and in one patient, a decrease in bone marrow [BM] blasts to <5%) were observed in 4 of the next 10 patients enrolled.  Except for neutropenic fever (n = 11), CEP-701-related toxicity was rare.  A second oral FLT3 inhibitor, PKC412 (IC50 = 10 nM), was studied by R. M. Stone and others in a phase II trial of relapsed or refractory mutant FLT3 AML.  PKC412 was administered at a dose of 75 mg TID and 12 of 14 patients experienced a >50% decrease in PB blasts while 5 patients had a >50% decrease in BM blasts (including one patient with <5% BM blasts).  Decreases in FLT3 autophosphorylation were found in 3 of 4 patient samples. Further study of these new agents is warranted. (Abstracts 779 and 2265)

 

CETUXIMAB

Metastatic colorectal cancer (MCRC).  D. Cunningham et al. conducted a study in which 329 patients with EGFR-positive irinotecan-refractory MCRC were randomized to receive the anti-EGFR antibody cetuximab (400 mg/m2 first infusion, then 250 mg/m2 weekly) plus irinotecan (at the same dose and regimen on which they had been progressing) (Arm A) or cetuximab alone (option to add irinotecan after failure of cetuximab as a single agent) (Arm B).  Arm A patients achieved a response rate of 17.9% and a median TTP of 126 days while those in Arm B had a response rate of 9.9% and a median TTP of 45 days.  Survival data is pending.  These data suggest an additive interaction for combination cetuximab/irinotecan therapy against MCRC. (Abstract 1012)

 

BEVACIZUMAB

Front-line therapy for advanced colorectal cancer (advCRC).  Bevacizumab (BEV) is a chimeric monoclonal antibody directed against VEGF that inhibits angiogenesis.  B. J. Giantonio and colleagues performed a phase II study in which previously untreated patients with measurable advCRC were treated with BEV (10 mg/kg every other week) plus irinotecan/5-FU/leucovorin (IFL) weekly for 4 weeks every 6 weeks.  After the first 20 patients, the starting doses of irinotecan and 5-FU were reduced to 100 mg/m2 (from 125 mg/m2) and 400 mg/m2 (from 500 mg/m2) due to a toxicity review of other IFL trials.  With a median follow-up of 7.6 months, a response (RECIST criteria) was achieved in 32 (45.7%) of 70 evaluable patients (2 [2.9%] CRs).  Of 83 patients evaluable for safety, grade 3 diarrhea occurred in 15 patients, one patient had grade 4 epistaxis, and 9 patients had a thrombotic event.  These findings suggest that BEV plus IFL has substantial antitumor activity in previously untreated patients with advCRC.  (Abstract 1024)

 

Phase III study of combination therapy with IFL.  The results of a phase III study in which 815 previously untreated patients with metastatic CRC were randomized to receive either BEV plus IFL or IFL alone were reported by Herbert Hurwitz et al.  Patients in the BEV treatment arm had a higher response rate (45% vs. 35%; p = 0.0029), a longer response duration (10.4 months vs. 7.1 months; p = 0.0014), a greater median time to tumor progression (10.6 vs. 6.2 months; p <0.00001), and an increased overall survival time (20.3 months vs. 15.6 months; p = 0.00003) compared to those patients treated with IFL alone.  The addition of BEV was well tolerated in combination with IFL chemotherapy.  Grade 3 hypertension developed in 10.9% of patients and was controlled with oral agents.  Although uncommon, gastrointestinal perforation was observed to occur only in BEV-treated patients.  These findings demonstrate that the combination of BEV and IFL therapy is tolerated with expectable toxicity and improves outcomes, including overall survival time, for previously untreated patients with metastatic CRC compared to IFL treatment alone.  (Abstract 3646) 

 

RITUXIMAB

Combined with CHOP for HIV-associated non-Hodgkin's lymphoma (NHL).  L.D. Kaplan and others from the AIDS Malignancies Consortium conducted a study in which patients with AIDS-associated aggressive B-cell NHL were randomized in a 2:1 ratio to receive standard CHOP plus rituximab (Arm A) or CHOP alone (Arm B).  All patients received G-CSF support.  The complete response rates for Arms A and B were 58% and 50%, respectively (p = 0.371).  Grade 3 or 4 neutropenia was reported in 39% of patients in Arm A and 17% of patients in Arm B (p =0.012).  Death due to infection occurred in 7% and 2% of Arm A and Arm B patients, respectively.  These preliminary data do not show a response benefit for combination therapy and suggest that the addition of rituximab to CHOP adds substantial toxicity in patients with AIDS-associated NHL.  (Abstract 2268)

 

Concurrent versus sequential treatment with FND chemotherapy (fludarabine, mitoxantrone, dexamethasone).  P. McLaughlin and associates at the M.D. Anderson Cancer Center randomized patients with stage IV indolent lymphoma to receive concurrent FND plus rituximab or sequential FND followed by rituximab.  All patients received maintenance interferon-alfa 2b (IFN) therapy for a year.  Eight 28-day cycles of FND (F - 25 mg/m2/day x 3; N - 10 mg/m2 on Day 1; D - 20 mg/m2/day x 5) were administered.  Six doses of rituximab 375 mg/m2 were given during the first 5 cycles of FND (concurrent arm) or with monthly maintenance IFN therapy (sequential arm).  Both schedules were tolerated well.  The preliminary results show no statistical differences between the concurrent and sequential arms for CR + CRu (92% vs. 85%), 3-year FFS rate (77% vs. 64%), and 3-year survival rate (95% vs. 95%).  (Abstract 2269)

 

Combination with hyper-CVAD in Burkitt (BL) and Burkitt-like (BLL) leukemia/lymphoma.  Cabanillas and coworkers at M.D. Anderson treated 20 patients with newly diagnosed BL or BLL with rituximab 375 mg/m2 on Days 1 and 11 of courses 1 and 3 of hyper-CVAD and Days 1 and 8 of courses 2 and 4 with high-dose methotrexate and ara-C.  The CR rate in 19 evaluable patients was 89%.  With a median follow-up of 12 months (range, 3-30+ months), 2 relapses have occurred.  Three deaths in HIV-BL patients in CR have occurred while 12 of 14 non-HIV patients (86%) remain alive and disease-free.  The safety profile was similar to that of hyper-CVAD alone and the addition of rituximab to hyper-CVAD may improve outcomes for patients with BL or BLL. (Abstract 2309)

 

BORTEZOMIB

Phase II studies in NHL.  O. A. O'Connor et al administered the proteosome inhibitor bortezomib (1.5 mg/m2 intravenously twice weekly for 2 weeks every 3 weeks) to 14 patients with relapsed or refractory indolent lymphomas in a phase II study.  Adverse events included thrombocytopenia and peripheral neuropathy (N = 2).  Seven patients have achieved objective responses (1 CR).  This trial is ongoing. In a second study, A. H. Goy et al. gave bortezomib 1.5 mg/m2 on Days 1, 4, 8, and 11 every 21 days to patients with relapsed or refractory indolent and aggressive B-cell NHL.  Data were available for 11 patients.  Four patients developed grade 3 or 4 gastrointestinal toxicity, 4 patients had grade 3 or 4 thrombocytopenia, and neuropathy occurred in one patient.  Five patients have achieved a response (1 CR; all responsive have been among 7 patients with mantle cell lymphoma).  These trials indicate that further study of bortezomib therapy in patients with NHL is warranted.  (Abstracts 2277 and 2291)

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