Anti-MUC1 antibody is a Human antibody of IgG4 κ class that binds to an MUC1.
Figure 1 Competitive radioimmunoassay for mCTM01 and hCTM01.
Affinity of the humanized antibody relative to the murine antibody is 1.3.
Hamann, P. R., Hinman, L. M., Beyer, C. F., Lindh, D., Upeslacis, J., Shochat, D., & Mountain, A. (2005). A calicheamicin conjugate with a fully humanized anti-MUC1 antibody shows potent antitumor effects in breast and ovarian tumor xenografts. Bioconjugate chemistry, 16(2), 354-360.
Figure 2 Internalization by MCF-7 (A) and A2780DDP (B) human cell lines.
Frame A shows the effect of humanization on uptake, while frame B shows the effect of conjugation to make CMB-401 on uptake of humanized antibody.
Hamann, P. R., Hinman, L. M., Beyer, C. F., Lindh, D., Upeslacis, J., Shochat, D., & Mountain, A. (2005). A calicheamicin conjugate with a fully humanized anti-MUC1 antibody shows potent antitumor effects in breast and ovarian tumor xenografts. Bioconjugate chemistry, 16(2), 354-360.
Figure 3 Response of OvCar-3.
Xenograft tumors were treated with CMB-401, the murine conjugate, or a representative calicheamicin derivative (6) alone. Athymic mice were implanted sc with OvCar-3 cells and then dosed when tumors were approximately 150 mg in size. The doses indicated were given on days 7, 11, and 15, as indicated by the arrows, and are given in calicheamicin equivalents. The corresponding concentration of antibody is 40-fold greater.
Hamann, P. R., Hinman, L. M., Beyer, C. F., Lindh, D., Upeslacis, J., Shochat, D., & Mountain, A. (2005). A calicheamicin conjugate with a fully humanized anti-MUC1 antibody shows potent antitumor effects in breast and ovarian tumor xenografts. Bioconjugate chemistry, 16(2), 354-360.
Figure 4 Effect of changing the fractionated dose IP to either a fractionated dose iv or to a bolus dose IP.
Athymic mice were implanted sc with MX-1 cells and then dosed with CMB-401 when tumors were approximately 150 mg in size. The doses indicated were given either on day 11, as indicated by the solid arrow (single dose), or on days 11, 15, and 19, as indicated by the open arrows, and are given in calicheamicin equivalents. The corresponding concentration of antibody is 40-fold greater. Error bars are SEMs.
Hamann, P. R., Hinman, L. M., Beyer, C. F., Lindh, D., Upeslacis, J., Shochat, D., & Mountain, A. (2005). A calicheamicin conjugate with a fully humanized anti-MUC1 antibody shows potent antitumor effects in breast and ovarian tumor xenografts. Bioconjugate chemistry, 16(2), 354-360.
Figure 5 Response of the MX-1 breast xenograft tumors.
Athymic mice were implanted sc with MX-1 cells and then dosed with the conjugates when tumors were approximately 150 mg in size. The control conjugate is an identical conjugate made with the nonbinding, isotype-matched antibody, P67.6. The doses indicated were given on days 11, 15, and 19 and are given in calicheamicin equivalents. The corresponding concentration of antibody is 40-fold greater. Error bars are SEMs and are given in the negative direction for the control conjugate and in the positive direction for CMB-401.
Hamann, P. R., Hinman, L. M., Beyer, C. F., Lindh, D., Upeslacis, J., Shochat, D., & Mountain, A. (2005). A calicheamicin conjugate with a fully humanized anti-MUC1 antibody shows potent antitumor effects in breast and ovarian tumor xenografts. Bioconjugate chemistry, 16(2), 354-360.
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