Disclosed are visible light-activatable antitumor self-assembled nanoparticles or antitumor immunity-inducing self-assembled nanoparticles. The self-assembled nanoparticles induce potent apoptosis in cancer cells and increase their own anticancer immunogenicity, thereby maximizing their therapeutic efficacy for cancer.

In one aspect, methods of targeted nanoparticles and cell delivery are described herein. In some embodiments methods described herein comprise coupling nanoparticles and cells to a carrier cell to form a nanoparticle-cell conjugate or cell-cell conjugate, disposing the nanoparticle-cell or cell-cell conjugate in a biological environment, and delivering the nanoparticles and cells to target cells or tissues located within the biological environment. The nanoparticles comprise a biodegradable photoluminescent polymer, and the nanoparticle-cell conjugate is formed using one or more click chemistry reaction products.

In one aspect, methods of targeted nanoparticles and cell delivery are described herein. In some embodiments methods described herein comprise coupling nanoparticles and cells to a carrier cell to form a nanoparticle-cell conjugate or cell-cell conjugate, disposing the nanoparticle-cell or cell-cell conjugate in a biological environment, and delivering the nanoparticles and cells to target cells or tissues located within the biological environment. The nanoparticles comprise a biodegradable photoluminescent polymer, and the nanoparticle-cell conjugate is formed using one or more click chemistry reaction products.

The present invention concerns novel and improved antibody-conjugates for targeting CD30. The inventors found that when antibody-conjugates were prepared using a specific mode of conjugation, they exhibit an improved therapeutic index. The mode of conjugation comprises a first step (i) of contacting a glycoprotein comprising 1-4 core N-acetylglucosamine moieties with a compound of the formula S(F.sup.1).sub.x-P in the presence of a catalyst, wherein S(F.sup.1).sub.x is a sugar derivative comprising x functional groups F.sup.1 capable of reacting with a functional group Q.sup.1, x is 1 or 2 and P is a nucleoside mono- or diphosphate, and wherein the catalyst is capable of transferring the S(F.sup.1).sub.x moiety to the core-GlcNAc moiety, to obtain a modified antibody; and a second step (ii) of reacting the modified antibody with a linker-conjugate comprising a functional group Q.sup.1 capable of reacting with functional group F.sup.1 and a target molecule D connected to Q.sup.1 via a linker L.sup.2 to obtain the antibody-conjugate wherein linker L comprises S—Z.sup.3-L.sup.2 and wherein Z.sup.3 is a connecting group resulting from the reaction between Q.sup.1 and F.sup.1. The invention also relates to a use for improving the therapeutic index of an antibody-conjugate and to a method for targeting CD30-expressing cells.

The present invention concerns novel and improved antibody-conjugates for targeting CD30. The inventors found that when antibody-conjugates were prepared using a specific mode of conjugation, they exhibit an improved therapeutic index. The mode of conjugation comprises a first step (i) of contacting a glycoprotein comprising 1-4 core N-acetylglucosamine moieties with a compound of the formula S(F.sup.1).sub.x-P in the presence of a catalyst, wherein S(F.sup.1).sub.x is a sugar derivative comprising x functional groups F.sup.1 capable of reacting with a functional group Q.sup.1, x is 1 or 2 and P is a nucleoside mono- or diphosphate, and wherein the catalyst is capable of transferring the S(F.sup.1).sub.x moiety to the core-GlcNAc moiety, to obtain a modified antibody; and a second step (ii) of reacting the modified antibody with a linker-conjugate comprising a functional group Q.sup.1 capable of reacting with functional group F.sup.1 and a target molecule D connected to Q.sup.1 via a linker L.sup.2 to obtain the antibody-conjugate wherein linker L comprises S—Z.sup.3-L.sup.2 and wherein Z.sup.3 is a connecting group resulting from the reaction between Q.sup.1 and F.sup.1. The invention also relates to a use for improving the therapeutic index of an antibody-conjugate and to a method for targeting CD30-expressing cells.

The present invention relates to an anti-MUC1 antibody binding specifically to Mucin 1 (MUC1) or an antigen-binding fragment thereof, an antibody-drug conjugate or bispecific antibody comprising the antibody, a pharmaceutical composition for prevention or treatment of cancer, comprising the same antibody, conjugate or bispecific antibody, and a nucleic acid encoding the same antibody, a vector and a host cell, both carrying the same nucleic acid, and a method for preparing an anti-MUC1 antibody or an antigen-binding fragment thereof, using the same vector and host cell. According to the present invention, the antibody shows outstanding affinity and binding force to MUC1 and the antibody-drug conjugate can bind specifically to a MUC1-expressing cell to specifically or selectively transfer the drug with efficacy. Therefore, the anti-MUC1 antibody and the antibody-drug conjugate according to the present invention can be usefully applied to the treatment of a MUC1-related disease, for example, cancer.

The present invention relates to an anti-MUC1 antibody binding specifically to Mucin 1 (MUC1) or an antigen-binding fragment thereof, an antibody-drug conjugate or bispecific antibody comprising the antibody, a pharmaceutical composition for prevention or treatment of cancer, comprising the same antibody, conjugate or bispecific antibody, and a nucleic acid encoding the same antibody, a vector and a host cell, both carrying the same nucleic acid, and a method for preparing an anti-MUC1 antibody or an antigen-binding fragment thereof, using the same vector and host cell. According to the present invention, the antibody shows outstanding affinity and binding force to MUC1 and the antibody-drug conjugate can bind specifically to a MUC1-expressing cell to specifically or selectively transfer the drug with efficacy. Therefore, the anti-MUC1 antibody and the antibody-drug conjugate according to the present invention can be usefully applied to the treatment of a MUC1-related disease, for example, cancer.

An anti-CEA antibody-exatecan analog conjugate and a pharmaceutical use thereof. Specifically, the anti-CEA antibody-exatecan analog conjugate is as shown in general formula (Pc-L-Y-D), wherein Pc is an anti-CEA antibody or an antigen-binding fragment thereof; L is a linker unit; Y is selected from —O—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O)—, —O—CR.sup.1R.sup.2—(CR.sup.aR.sup.b).sub.m—, —O—CR.sup.1R.sup.2—, —NH—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O)—, and —S—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O); and n is a decimal or integer from 1 to 10.

##STR00001##

An anti-CEA antibody-exatecan analog conjugate and a pharmaceutical use thereof. Specifically, the anti-CEA antibody-exatecan analog conjugate is as shown in general formula (Pc-L-Y-D), wherein Pc is an anti-CEA antibody or an antigen-binding fragment thereof; L is a linker unit; Y is selected from —O—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O)—, —O—CR.sup.1R.sup.2—(CR.sup.aR.sup.b).sub.m—, —O—CR.sup.1R.sup.2—, —NH—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O)—, and —S—(CR.sup.aR.sup.b).sub.m—CR.sup.1R.sup.2—C(O); and n is a decimal or integer from 1 to 10.

##STR00001##

The present invention provides an agent for adjuvant therapy of tumors that exerts remarkable inhibitory effects on tumor metastasis and recurrence while developing few side effects. The agent for adjuvant therapy comprises, as an active ingredient, a peptide having 4 linked CTL epitopes.