Activators & Inhibitors

Insulin efsitora alfa (LY-3209590) is a selective insulin receptor (IR) agonist, featuring a fusion protein that combines human IR agonists with the crystallizable (Fc) domain of human immunoglobulin G2 (IgG2), and has a molecular weight of 64.1 kDa. This compound is well tolerated and shows promise for diabetes management [1].

Ipafricept (OMP-54F28; FZD8-Fc) is a pioneering recombinant fusion protein composed of the extracellular segment of the human frizzled-8 receptor and the Fc fragment of human IgG1, targeting the Wnt ligand. It demonstrates activity in inhibiting solid tumors and is well tolerated [1].

Latikafusp (AMG 256), a bifunctional fusion protein, combines a PD-1-targeting antibody with an IL-21 mutein, facilitating IL-21 pathway stimulation in PD-1+ cells. It aims to enhance and sustain the functionality of cytotoxic and memory T cells, thereby inducing anti-tumor immunity. This compound shows promise for research in solid tumors [1] [2].

Nemvaleukin alfa (ALKS 4230), an IL-2 fusion protein, selectively targets intermediate-affinity IL-2R to activate NK and effector T cells, and is used in cancer research [1] [2] [3].

Recifercept (TA-46), a soluble, recombinant fibroblast growth factor receptor 3 (FGFR3) molecule, serves as a decoy/ligand trap to diminish the binding of fibroblast growth factors to mutant FGFR3 receptors. Primarily, it is utilized in achondroplasia research [1].

Simlukafusp alfa (FAP-IL2v) is an immunocytokine consisting of an antibody targeting fibroblast activation protein α (FAPα) linked to a variant of IL-2 that specifically interacts with IL-2Rβγ. The compound is of the human IgG1 isotype [1].

Vantictumab (OMP-18R5), a fully human IgG2 monoclonal antibody, antagonizes Wnt pathway signaling through binding to FZD1/2/5/7/8 receptors. It is currently under investigation for the treatment of various cancers, including metastatic HER2-negative breast cancer and metastatic pancreatic adenocarcinoma [1] [2].

Sacituzumab govitecan (IMMU-132), an antibody-drug conjugate (ADC) targeting Trop-2, facilitates the delivery of SN-38. It demonstrates anticancer activity [1].

Telisotuzumab vedotin (ABBV-399), an antibody-drug conjugate (ADCs), targets c-Met and comprises the cytotoxic agent Monomethyl Auristatin E (MMAE), the Telisotuzumab antibody, and a cleavable mc-val-cit-PABC linker. This compound is utilized in cancer research [1].