ONC

Oral second-generation Bruton's tyrosine kinase inhibitor (Calquence). Approved in chronic lymphocytic leukemia, mantle cell lymphoma, and small lymphocytic lymphoma.

Bendamustine is a bifunctional mechlorethamine derivative containing a purine-like benzimidazole ring. Mechlorethamine and its derivatives form electrophilic alkyl groups.

Oral chimeric BTK degrader (BeiGene) targeting BTK including ibrutinib-resistant mutations. Phase 3 in chronic lymphocytic leukemia and other B-cell malignancies.

Oral 5-fluorouracil prodrug activated to 5-FU in tumor tissue. Used in colorectal, breast, and gastric cancers, often combined with oxaliplatin or platinum.

Platinum-based chemotherapy that forms DNA crosslinks. Foundational cytotoxic agent used across testicular, bladder, ovarian, head and neck, and lung cancers.

Fruquintinib is a small molecule kinase inhibitor of vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3 with IC 50 values of 33, 35, and 0.5 nM, respectively.

Idelalisib is an inhibitor of phosphatidylinositol 3-kinase, PI3Kδ, which is expressed in normal and malignant B-cells. Idelalisib induced apoptosis and inhibited proliferation in cell lines derived from malignant B-cells and in primary tumor cells.

Lenvatinib is a kinase inhibitor that inhibits the kinase activities of vascular endothelial growth factor (VEGF) receptors VEGFR1 (FLT1), VEGFR2 (KDR), and VEGFR3 (FLT4).

Reduced folate used to rescue normal cells from methotrexate toxicity and to potentiate 5-FU activity (FOLFOX, FOLFIRI). Not a primary anticancer agent.

Bupivacaine blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential.

Glycoengineered Type II anti-CD20 monoclonal antibody (Gazyva) with enhanced ADCC. Approved in chronic lymphocytic leukemia and follicular lymphoma.

Third-generation platinum chemotherapy that forms DNA adducts. Backbone in colorectal cancer (FOLFOX) and other GI malignancies.

Pirtobrutinib is a small molecule, noncovalent inhibitor of BTK. BTK is a signaling protein of the B-cell antigen receptor (BCR) and cytokine receptor pathways.

Chimeric anti-CD20 monoclonal antibody (Rituxan) that depletes B cells via ADCC, CDC, and apoptosis. Foundational in B-cell lymphomas, CLL, rheumatoid arthritis, and ANCA vasculitis.

Oral next-generation selective BCL-2 inhibitor (BeiGene) with improved potency and shorter half-life vs venetoclax. Phase 3 in chronic lymphocytic leukemia and Waldenström macroglobulinemia.

Oral DNA-methylating chemotherapy that crosses the blood-brain barrier. Standard of care in glioblastoma multiforme; also used in melanoma.

Anti-PD-1 monoclonal antibody (Tevimbra) engineered to minimize FcγR binding. Approved in esophageal squamous cell carcinoma, NSCLC, and other cancers.

Oral selective BCL-2 inhibitor (Venclexta) that restores apoptosis in cancer cells. Approved for chronic lymphocytic leukemia, acute myeloid leukemia, and small lymphocytic lymphoma.

Biparatopic anti-HER2 bispecific antibody (Ziihera) that binds two distinct HER2 epitopes simultaneously, enhancing receptor clustering and signal disruption. Approved in HER2-positive biliary tract cancer.

Oral second-generation BTK inhibitor (Brukinsa) with reduced off-target effects vs ibrutinib. Approved in chronic lymphocytic leukemia, mantle cell lymphoma, and Waldenström macroglobulinemia.

Tacrolimus binds to an intracellular protein, FKBP-12. A complex of tacrolimus-FKBP-12, calcium, calmodulin, and calcineurin (a ubiquitous mammalian intracellular enzyme) is then formed and the phosphatase activity of calcineurin is inhibited.

Carfilzomib is a tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds to the N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome.

Anti-CD38 monoclonal antibody (Darzalex). Approved across multiple myeloma settings; subcutaneous formulation marketed as Darzalex Faspro.

Synthetic corticosteroid widely used as anti-inflammatory and immunosuppressant. In oncology, used in multiple myeloma regimens and as supportive care for chemotherapy-induced nausea/edema.

Glofitamab-gxbm is a bispecific antibody that binds to CD20 expressed on the surface of B cells, and to CD3 receptor expressed on the surface of T cells. Glofitamab-gxbm causes T-cell activation and proliferation, secretion of cytokines, and the lysis of CD20-expressing B cells.

Mosunetuzumab-axgb is a T-cell engaging bispecific antibody that binds to the CD3 receptor expressed on the surface of T-cells and CD20 expressed on the surface of lymphoma cells and some healthy B-lineage cells.

Pomalidomide is an analogue of thalidomide with immunomodulatory, antiangiogenic, and antineoplastic properties. Cellular activities of pomalidomide are mediated through its target cereblon, a component of a cullin ring E3 ubiquitin ligase enzyme complex.