临床前 1a期 1b期 2期 3期/确证性

Hematology Franchise

Zynlonta™ (loncastuximab tesirine-lpyl)
Targeting CD19

Loncastuximab Tesirine (ADCT-402, Lonca) Targeting CD19

Lonca is an ADC composed of a humanized monoclonal antibody that binds to human CD19 and conjugated through a linker to a PBD-dimer toxin. Once bound to a CD19-expressing cell, Lonca is internalized into the cell where enzymes release the PBD-based warhead.

CD19 is an ideal target for an ADC approach

CD19 is highly expressed in a range of B-cell hematological tumors, including certain types of lymphoma and leukemia, while its expression in healthy tissue is restricted.

Lonca is the focus of the LOTIS Clinical Development Program

In clinical trials, lead candidate Lonca has demonstrated significant single-agent clinical activity across a broad population of patients with relapsed or refractory diffuse large B-cell, mantle cell, and follicular lymphomas.

Diffuse Large B-Cell Lymphoma (US)
FDA Approved
Diffuse Large B-Cell Lymphoma (China)
Pivotal
Diffuse Large B-Cell Lymphoma and Mantle Cell
Lymphoma, in combination with ibrutinib
Pivotal
Follicular Lymphoma
Pivotal

ADCT-602 Targeting CD22

ADCT-602 targeting CD22

ADCT-602 is an ADC composed of a monoclonal antibody that binds to CD22 conjugated to a PBD–dimer toxin. Once bound to a CD22-expressing cell, ADCT-602 is internalized into the cell where enzymes release the PBD-based warhead. CD22 is an attractive and clinically validated ADC target. CD22 is highly expressed on most malignant B-cells, including expression in more than 90% of patients with B-cell acute lymphoblastic leukemia (ALL).

ADCT-602 is being evaluated in a phase I/II clinical trial in patients with relapsed or refractory B-cell ALL (NCT03698552). The trial is being led by The University of Texas MD Anderson Cancer Center.

leuke mia Acute Lymphoblastic Leukemia

Solid Tumor Franchise

Mipasetamab Uzoptirine (ADCT-601)
Targeting AXL

ADCT-601 targeting AXL

ADCT-601 is an ADC composed of a humanized monoclonal antibody that binds to human AXL (licensed from BerGenBio), conjugated using GlycoConnect™ technology (licensed from Synaffix BV) to a linker with a PBD–dimer toxin. Once bound to an AXL-expressing cell, ADCT-601 is internalized into the cell, where enzymes release the PBD-based warhead. AXL is an ideal target for an ADC approach, as it is highly overexpressed in many solid tumors (eg, lung, breast, prostate, pancreas, glioma, and esophageal) and hematological malignancies (eg, acute and chronic myeloid leukemia).

ADCT-601 is being evaluated in a phase 1 clinical trial in patients with selected advanced solid tumors (NCT03700294).


Various Solid Tumors

ADCT-901
Targeting KAAG1

ADCT-901 targeting KAAG1

ADCT-901 is an ADC composed of a humanized monoclonal antibody (3A4) directed against human KAAG1 and conjugated through a cathepsin-cleavable linker to SG3199, a PBD–dimer cytotoxin. KAAG1 is an attractive novel tumor target for ADC development as (i) it is an intracellular target by definition, but becomes exposed on the membrane of tumor cells, (ii) it has high expression in tumors with high unmet medical need, including ovarian cancer and triple negative breast cancer, while its expression on healthy tissue is very restricted, and (iii) it internalizes and co-localizes with lysosomal-associated membrane protein 1, a lysosomal marker, which shows that the target is efficiently transported to the cellular compartment where efficient release of the cytotoxin is expected.

ADCT-901 is being developed for the treatment of advanced solid tumors with high unmet medical needs, including platinum resistant ovarian cancer and triple negative breast cancer.

Various Solid Tumors