Drugs intended to be endocytosed by macrophages may be transported by MAbs directed against these cells. Twenty MAbs were investigated for this purpose. The binding of these MAbs to macrophages obtained from a 7 day culture of blood monocytes showed that anti-CD11b and anti-CD14 recognized the highest number of cell surface antigen sites. Further assays determined that anti-CD63, Mo5 and anti-CD33 were the MAbs that induced the strongest modulation of the corresponding antigens, the highest rate being with anti-CD63. Endocytosis of antigen-antibody complexes was evidenced by the presence of MAbs in the cytoplasm. Anti-CD63 MAbs induced the highest internalization in this assay. For most MAbs, however, the density of antigen sites and the intensity of antigen modulation were not predictive of the amount of MAb detected in the cytoplasm.