BioOncology Watch

Timely Information for Practicing Physicians

 

march 2003

RITUXIMAB

Complement-dependent cytotoxicity (CDC).  Rituximab activates complement when it binds to CD20+ B-cells and the resulting cell-surface deposition of complement fragment protein (C3b and its breakdown products (C3b[i]) may opsonize cells for destruction.  Adam Kennedy and colleagues at the University of Virginia Health Sciences Center (Charlottesville) found that the incubation of CD20+ cells with an anti-C3b[i] monoclonal antibody (mAb 3E7) in addition to rituximab in normal human serum enhanced C3b[i] deposition.  Furthermore, rituximab-mediated killing of both Raji and DB cells was enhanced by mAb 3E7.  A second set of experiments by Olivier Manches et al.  (Michallon Hospital, Grenoble, France) examined rituximab-mediated killing mechanisms on freshly-obtained patient-derived lymphoma cells.  They observed rituximab-related CDC lysis to be high in follicular lymphoma cells, moderate in large cell and mantle cell lymphoma cells, and low to non-existent in small lymphocytic lymphoma cells.  In general, these findings are consistent with the reported response rates of different subgroups of lymphoma to rituximab therapy.  These studies suggest that complement plays a key role in the mechanism of action of rituximab against lymphoma.  (Kennedy AD, et al. Blood 2003;101:1071-1079 and Manches O, et al. Blood 2003;101:949-954)

 

ADOPTIVE IMMUNOTHERAPY

Antileukemic activity of allorestricted cytotoxic T lymphocytes (CTLs).  Allorestricted CTLs directed against CD45 can recognize host leukemia cells but not donor cells from a marrow graft or host non-hematopoietic tissues.  Persis Amrolia and associates identified four CD45-derived peptides that showed binding to HLA-A0201.  Only one of these peptides, P1218, was able to generate peptide-specific CTL lines (from 3 of 7 donors).  The P1218-specific CTL lines recognized leukemic blasts obtained from patients with chronic or acute myeloid leukemias and were active against hematopoietic cell lines expressing both HLA-A2 and CD45, but were not cytotoxic to CD45-negative or HLA-A2-negative cells.  P1218-specific CTLs have potent activity against leukemic progenitor cells and may contribute to host myeloablation, thus enhancing donor cell engraftment.  P1218-specific CTL lines can be easily expanded for clinical protocols. (Amrolia PJ, et al. Blood 2003;101:1007-1014)

 

PHASE I AND II TRIALS

Phase I study of cantuzumab mertansine.  Anthony Tolcher and colleagues conducted a phase I study of escalating doses (22 to 295 mg/m2) of cantuzumab mertansine administered intravenously (i.v.) every 3 weeks to chemotherapy-refractory patients with CanAg-expressing solid malignancies (N = 37).  Cantuzumab mertansine (GlaxoSmithKline and ImmunoGen Inc.) is a novel tumor-activated immunoconjugate made up of the maytansine derivative DM1 (an antimicrotubule agent) linked to the humanized monoclonal antibody huC242 that is directed against the extracellular epitope of CanAg (a glycoform of MUC1).  CanAg is strongly expressed in most pancreatic, biliary, and colorectal cancers as well as a number of non-small cell lung, gastric, uterine, and bladder cancers.  The immunoconjugate complex is internalized following the binding of cantuzumab mertansine to the external domain of CanAg and the DM1-huC242 disulfide linkage is then cleaved releasing DM1 molecules intracellularly.  The maximum tolerated dose (MTD) was determined to be 235 mg/m2 i.v. every 3 weeks and dose-limiting toxicities (DLTs) were grade 3 liver transaminase elevations and grade 3 fatigue.  Dose, peak concentration, and area under the concentration-time curve correlated with the severity of transaminase elevation.  Shed CanAg plasma levels decreased to undetectable levels in 25 of 30 patients after the first dose of cantuzumab mertansine.  Minor tumor responses were observed in 2 colorectal carcinoma patients and 4 patients had stable disease for >6 courses.  These encouraging results warrant further investigation of this agent in CanAg-expressing tumors.  (Tolcher AW, et al. J Clin Oncol 2003;21:211-222)

 

Phase II study of trastuzumab in gynecologic tumors.  Michael Bookman and associates of the Gynecologic Oncology Group (GOG) performed a phase II trial that evaluated trastuzumab (HerceptinÒ; Genentech Inc) monotherapy in previously treated patients with ovarian or primary peritoneal carcinoma that had HER2 overexpression (2+ or 3+).  Only 95 patients (11.4%) out of 837 patients screened exhibited the requisite level of HER2 overexpression.  Of these, 45 patients were enrolled into the study.  Among 41 evaluable patients, a response rate of 7.3% (1 complete and 2 partial responses) was achieved with i.v. trastuzumab treatments (induction dose of 4 mg/kg followed by 2 mg/kg weekly).  Trastuzumab-related toxicities were mild in severity.  These findings demonstrate that HER2 overexpression is infrequent in ovarian and primary peritoneal carcinomas and that trastuzumab has limited activity in these gynecologic tumors.  (Bookman MA, et al. J Clin Oncol 2003;21:283-290)

 

PROTEASOME INHIBITOR

Molecular mechanisms of activity.  The ubiquitin-proteasome pathway regulates cell-cycle progression by regulating cyclins and cyclin-dependent kinase inhibitor proteins.  The recently developed proteasome inhibitor, PS-341, has been previously shown to induce apoptosis in resistant multiple myeloma (MM) cells, inhibit adhesion of MM cells, and inhibit MM growth-promoting cytokines.  Teru Hideshima and coworkers from the Dana Farber Cancer Institute (Boston, MA) now report that studies utilizing MM-derived cell lines and fresh patient-derived MM cells demonstrate that PS-341 induces caspase-8 and -3 activity through the activation of JNK, inhibits DNA repair, and activates p53 by phosphorylation and degradation of MDM2 protein.  These studies provide a framework for further evaluation of PS-341.  (Blood 2003;101:1530-1534)

 

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