A drug delivery molecule, comprising: a targeting moiety that significantly binds to a receptor on a surface of a cell, and wherein binding of the targeting moiety to the receptor results in an uptake of the drug delivery molecule into the cell; a routing moiety selected from a nuclear translocation signal sequence, a cytoplasmatic retention signal, an endoplasmatic reticulum export signal or a mitochondrial translocation signal; and a bioactive molecule, coupled to the routing moiety, wherein at least one of the routing moiety and the bioactive molecule is coupled to the targeting moiety; and wherein the bioactive molecule comprises a drug or prodrug, said BAM further comprising one out of a short peptide sequence that is a substrate for an intracellular protease, a disulfide bond, a charge-complementary coupling, an ionic/coordinating interaction, a hydrogen bond, a hydrophobic interaction; or the BAM is a non-drug, non-prodrug reporter group that can be used for diagnostic purposes; and wherein the targeting moiety (i) comprises a somatostatin analog that significantly binds to a polypeptide hormone receptor on a surface of a cell; or (ii) comprises a natural or synthetic fragment of the natural ligand of a polypeptide receptor or is a molecule homologous to a portion of the natural ligand, and significantly binds to the polypeptide receptor on a surface of a cell wherein the polypeptide receptor is a neurotransmitter receptor or a hormone receptor or a growth factor receptor. a targeting moiety that significantly binds to a receptor on a surface of a cell, and wherein binding of the targeting moiety to the receptor results in an uptake of the drug delivery molecule into the cell; a routing moiety selected from a nuclear translocation signal sequence, a cytoplasmatic retention signal, an endoplasmatic reticulum export signal or a mitochondrial translocation signal; and a bioactive molecule, coupled to the routing moiety, wherein at least one of the routing moiety and the bioactive molecule is coupled to the targeting moiety; and wherein the bioactive molecule comprises a drug or prodrug, said BAM further comprising one out of a short peptide sequence that is a substrate for an intracellular protease, a disulfide bond, a charge-complementary coupling, an ionic/coordinating interaction, a hydrogen bond, a hydrophobic interaction; or the BAM is a non-drug, non-prodrug reporter group that can be used for diagnostic purposes; and wherein the targeting moiety (i) comprises a somatostatin analog that significantly binds to a polypeptide hormone receptor on a surface of a cell; or (ii) comprises a natural or synthetic fragment of the natural ligand of a polypeptide receptor or is a molecule homologous to a portion of the natural ligand, and significantly binds to the polypeptide receptor on a surface of a cell wherein the polypeptide receptor is a neurotransmitter receptor or a hormone receptor or a growth factor receptor. (i) comprises a somatostatin analog that significantly binds to a polypeptide hormone receptor on a surface of a cell; or (ii) comprises a natural or synthetic fragment of the natural ligand of a polypeptide receptor or is a molecule homologous to a portion of the natural ligand, and significantly binds to the polypeptide receptor on a surface of a cell wherein the polypeptide receptor is a neurotransmitter receptor or a hormone receptor or a growth factor receptor.