advanced malignancies

Aplidine possesses antiviral activity against SARS-CoV-2(IC90 = 0.88 nM). Aplidine is a potent anti-cancer agent by targeting eukaryotic translation elongation factor 1 Alpha 2(EEF1A2, Kd = 80 nM).

GAC0003A4 is a potent LXR inverse agonist with antitumor activity that inhibits the transcription of LXR proteins.GAC0003A4 degrades LXRβ proteins and inhibits the proliferation of PDAC cells in a dose-dependent manner.GAC0003A4 has been used in the study of advanced pancreatic cancers and other recalcitrant malignancies.

BAY1238097, a potent and selective bromodomain and extra-terminal motif (BET) inhibitor with anticancer activity, exhibits strong antiproliferative effects in AML (Acute Myeloid Leukemia) and MM (Multiple Myeloma) models. BAY1238097 is useful for studying advanced refractory malignancies.

Tefinostat (CHR-2845) is a potent monocyte/macrophage-targeted histone deacetylase (HDAC) inhibitor that is cleaved to the active acid CHR-2847 by intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat exhibits antitumor activity and can be used in the study of leukemia and advanced hematologic malignancies.

ASP3026 has been used in trials studying the treatment of Solid Tumor, B-Cell Lymphoma, Advanced Malignancies, Positive for Anaplastic Lymphoma Kinase, and Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS.

BMS-599626 (AC480) has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.

CCT241736 is an orally bioavailable dual FLT3/Aurora kinase inhibitor that also inhibits clinically relevant FLT3-resistant mutants including FLT3-ITD and FLT3, CCT241736, an advanced analog of CCT137690, is a preclinical development candidate for the treatment of human malignancies, and in particular AML in adults and children.

FX-909 is a covalent peroxisome proliferator–activated receptor gamma (PPARγ) inverse agonist developed for advanced solid malignancies, including muscle-invasive bladder cancer, and functional profiling and NMR studies demonstrate that FX-909 exhibits enhanced corepressor-selective inverse agonism and superior stabilization of a transcriptionally repressive PPARγ ligand-binding domain conformation compared with T0070907.

Utomilumab (PF 05082566) is a humanized IgG2 antibody that targets the T-cell co-stimulatory receptor 4-1BB/CD137 and acts as a 4-1BB/CD137 agonist. It exhibits antitumor activity and may be used in the study of patients with advanced malignancies.

Betifisolimab (MSB-2311), a humanized monoclonal antibody targeting the immunosuppressive ligand PD-L1, shows promise for research in advanced solid tumors and hematological malignancies [1].

Finotonlimab is a highly specialized recombinant humanized monoclonal antibody of the immunoglobulin G4 isotype target the human programmed cell death protein 1 receptor with exceptional binding affinity and selectivity, restoration of T-lymphocyte mediated anti-tumor immunity by disrupting the inhibitory signaling axis established through interactions with PD-L1 and PD-L2 ligands across various preclinical and clinical experimental models of advanced solid malignancies.

Toripalimab is a recombinant, humanized immunoglobulin G4 (IgG4) monoclonal antibody that specifically targets and blocks the programmed cell death protein 1 (PD-1) immune checkpoint receptor, thereby acting as an immune checkpoint inhibitor used in clinical research for the investigation of advanced or metastatic malignancies, most notably nasopharyngeal carcinoma.

Surzebiclimab (BGB-A425) is a humanized monoclonal antibody specifically targeting TIM-3 (T-cell immunoglobulin and mucin domain containing -3), exhibiting high affinity (KD=0.36 nM) for the extracellular domain of human TIM-3. It is applicable for investigating advanced malignancies.

AZD-9574 is a selective inhibitor of PARP1 at the sites of SSBs. AZD-9574 exhibits anti-cancer activities and can be used in studies about HRD+ breast cancer and advanced solid malignancies.