microtubule-targeted

Maytansine (NSC-153858), an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata, inhibits the assembly of microtubules by binding to tubulin at the rhizoxin binding site.

Eribulin mesylate (E7389 mesylate) belongs to natural product derivatives and is a microtubule-targeted anticancer agent, functioning as a microtubule dynamics inhibitor that suppresses tubulin polymerization through tubulin binding, with cell permeability. This drug is used for the treatment of metastatic breast cancer.

Mal-PEG2-VCP-Eribulin is a chemotherapeutic compound comprising an antibody-drug conjugate (ADC) linker (Mal-PEG2-VCP) and the microtubule inhibitor Eribulin[1]. This compound uniquely targets microtubules, offering a novel approach to cancer treatment. Eribulin is specifically utilized in creating targeted Eribulin-based drugs for antibody conjugates[1].

Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a microtubule polymerization inhibitor prodrug mediated by Pd. Developed from colchicine-binding site inhibitors (CBSIs), it aims to reduce toxicity and enhance targeted release. Compared to the parent compound, its cytotoxicity is decreased by 68.3 times, but can be in situ restored in the presence of Pd resin. Mechanistic studies show it retains the same antitumor activity as CBSIs. In vivo tests demonstrate that, once activated by Pd resin, it significantly suppresses tumor growth (63.2% inhibition rate). Tubulin Polymerization-IN-1 prodrug is a promising candidate for cancer research.

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody–drug conjugate that combines the HER2-targeted antitumor specificity of trastuzumab with the potent cytotoxic activity of the microtubule inhibitor DM1, Trastuzumab emtansine enables selective intracellular delivery of the cytotoxic payload to HER2-expressing cells and supporting translational and mechanistic research in advanced breast cancer models.

Epofolate is folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Zilovertamab vedotin is a novel antibody-drug conjugate (ADC) constructed by conjugating the humanized monoclonal antibody zilovertamab with the anti-microtubule cytotoxic drug monomethyl vedotin. It binds to ROR1 on the surface of tumor cells, promotes rapid internalization and trafficking of the complex to lysosomes, followed by ADC cleavage and release of monomethyl vedotin, thereby inducing tumor cell apoptosis. It can be used in cancer-related research.

Naratuximab emtansine (IMGN529) is a CD37-targeted antibody-drug conjugate (ADC) composed of a humanized IgG1 monoclonal antibody linked to the microtubule-disrupting agent DM1. This compound demonstrates high affinity and specificity to CD37, facilitating the internalization, processing, and intracellular release of DM1. The functional activity of DM1 enables it to induce cell cycle arrest and apoptosis by disrupting microtubule assembly.

Mertansine-¹³C,d₃ (DM1-¹³C,d₃) is a ¹³C and deuterium-labeled form of Mertansine. Mertansine (DM1) is a microtubule inhibitor and a conjugatable maytansinoid alkaloid intended to reduce systemic toxicity associated with maytansinoids and improve tumor-targeted delivery. It can be conjugated to monoclonal antibodies through linker molecules to form antibody-drug conjugates (ADCs).

Epothilone D is a natural polyketide compound isolated from the myxobacterium Sorangium cellulosum that binds to tubulin and inhibits microtubule disassembly, thereby blocking mitosis, cellular proliferation, and cell motility, Epothilone D is extensively utilized in cancer research to study microtubule dynamics, mitotic arrest, and cytoskeleton-targeted anticancer mechanisms.