# US 2026/0097129 A1 · Antibody-drug conjugate comprising drug and antibody specifically binding to grp94 or antigen-binding fragment thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 2026/0097129 A1 - Document ID: US20260097129A1 - Status: Published application - Kind: A1 - Application number: 19/114,039 - Filed: 2023-09-25 - Published: 2026-04-09 - Earliest claimed: 2022-09-23 - Assignees: Kookmin University Industry Academy Cooperation Foundation - Applicants: Kookmin University Industry Academy Cooperation Foundation - Inventors: Sukmook LEE; Yea Bin CHO; Ji Woong KIM; Kyun HEO; Hyun Jung KIM - Web page: https://patentgrep.com/patent/US20260097129A1 ## CPC - A61K 47/68033: {the drug being a maytansine} - A61K 31/5365: ortho- or peri-condensed with heterocyclic ring systems - A61K 47/6843: {the antibody targeting a material from animals or humans} - A61K 47/6849: {the antibody targeting a receptor, a cell surface antigen or a cell surface determinant} - A61K 47/6863: {the tumour determinant being from stomach or intestines cancer cell} - A61P 35/00: Antineoplastic agents - A61P 35/04: specific for metastasis - C07K 16/18: against material from animals or humans - C12N 15/85: for animal cells - C07K 2317/77: Internalization into the cell - C07K 2317/92: Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) - C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00) ## Abstract The present invention relates to: an antibody-drug conjugate comprising a drug and an antibody specifically binding to GRP94 or an antigen-binding fragment thereof; and a pharmaceutical composition for treating cancer, comprising same as an active ingredient. The antibody-drug conjugate of the present invention comprises an antibody specifically targeting GRP94 and having strong internalization activity, and, as a result of conjugation with a cytotoxic agent, effectively inhibits the growth of cetuximab-resistant CRC cell lines including HT29, HCT116, HCT8 and LoVo cells, and thus can be effectively used as a therapeutic agent for various carcinomas in which GRP94 is overexpressed. ## Claims ### Claim 1 An antibody-drug conjugate (ADC) comprising an antibody or an antigen-binding fragment thereof that specifically binds to GRP94, and a drug, wherein the antibody or antigen-binding fragment thereof comprises: (i) a heavy chain complementarity-determining region 1 (HCDR1) comprising the amino acid sequence of SEQ ID NO: 1, a heavy chain complementarity-determining region 2 (HCDR2) comprising the amino acid sequence of SEQ ID NO: 2, a heavy chain complementarity-determining region 3 (HCDR3) comprising the amino acid sequence of SEQ ID NO: 3, a light chain complementarity-determining region 1 (LCDR1) comprising the amino acid sequence of SEQ ID NO: 4, a light chain complementarity-determining region 2 (LCDR2) comprising the amino acid sequence of SEQ ID NO: 5, and a light chain complementarity-determining region 3 (LCDR3) comprising the amino acid sequence of SEQ ID NO: 6; or (ii) a HCDR1 comprising the amino acid sequence of SEQ ID NO: 9, a HCDR2 comprising the amino acid sequence of SEQ ID NO: 10, a HCDR3 comprising the amino acid sequence of SEQ ID NO: 11, a LCDR1 comprising the amino acid sequence of SEQ ID NO: 12, a LCDR2 comprising the amino acid sequence of SEQ ID NO: 13, and a LCDR3 comprising the amino acid sequence of SEQ ID NO: 14. ### Claim 2 (depends on 1) The antibody-drug conjugate of claim 1, wherein the antibody or antigen-binding fragment thereof of (i) comprises a heavy chain variable region comprising the amino acid sequence of SEQ ID NO: 7 and a light chain variable region comprising the amino acid sequence of SEQ ID NO: 8. ### Claim 3 (depends on 1) The antibody-drug conjugate of claim 1, wherein the antibody or antigen-binding fragment thereof of (ii) comprises a heavy chain variable region comprising the amino acid sequence of SEQ ID NO: 15 and a light chain variable region comprising the amino acid sequence of SEQ ID NO: 16. ### Claim 4 (depends on 1) The antibody-drug conjugate of claim 1, wherein the antibody or antigen-binding fragment thereof in (i) or (ii) binds to a GRP94 target antigen expressed on the cell membrane or within the cell membrane of cancer cells, and the antibody, after binding to the GRP94 target antigen, is internalized into the cell. ### Claim 5 (depends on 1) The antibody-drug conjugate of claim 1, wherein the antibody or antigen-binding fragment thereof comprises selenocysteine in the constant region. ### Claim 6 (depends on 5) The antibody-drug conjugate of claim 5, wherein the drug is conjugated to the selenocysteine. ### Claim 7 (depends on 1) The antibody-drug conjugate of claim 1, wherein the drug is conjugated to a lysine residue of the antibody. ### Claim 8 (depends on 1) The antibody-drug conjugate of claim 1, further comprising a linker that connects the antibody or antigen-binding fragment thereof and the drug. ### Claim 9 (depends on 1) The antibody-drug conjugate of claim 1, wherein the drug is a maytansinoid. ### Claim 10 (depends on 1) The antibody-drug conjugate of claim 1, comprising 1 to 20 units of the drug per antibody or antigen-binding fragment thereof. ### Claim 11 (depends on 1) A pharmaceutical composition for treating cancer, inhibiting cancer metastasis, or inhibiting angiogenesis, comprising the antibody-drug conjugate of claim 1. ### Claim 12 (depends on 11) The pharmaceutical composition of claim 11, wherein the cancer comprises one or more cells that express GRP94 at elevated levels compared to non-cancerous cells. ### Claim 13 (depends on 1) A method for treating cancer, inhibiting cancer metastasis, or inhibiting angiogenesis, the method comprising: administering to a subject in need thereof a pharmaceutical composition comprising the antibody-drug conjugate of claim 1.