Anhydrovinblastine (AVLB) is a semisynthetic vinca alkaloid, which can safely be administered every 3 weeks at a dose of 21 mg/m2. Anhydrovinblastine is a cell cycle-specific anti-mitotic agent whose anti-tumour activity is directly related to its ability to bind tightly to tubulin and inhibit its polymerization into microtubules. Anhydrovinblastine has been used in trials studying the treatment of adult solid rumor, but this research has been discontinued.

Erbulozole (R 55104) is a water soluble congener of the microtubule inhibitor tubulozole, which has proven to possess anti-invasive, antitumoral and radiosensitizing capacities. Erbulozole development for the treatment of cancer has been discontinued.

Carbendazim is a broad-spectrum benzimidazole antifungal with potential antimitotic and antineoplastic activities widely used as a fungicide in agriculture and home gardening, and as an antihelminthic in veterinary medicine. As a fungicide, carbendazim used for controls Ascomycetes, Fungi Imperfecti, and Basidiomycetes on a wide variety of crops, including bananas, cereals, cotton, fruits, grapes, mushrooms, ornamentals, peanuts, sugarbeet, soybeans, tobacco, and vegetables. Carbendazim is a chemically stable and relatively persistent fungicide which only metabolizes to a limited extent in plants and in soil. The only detected metabolite is 2-aminobenzimidazole, which constitutes less than 5% of the total residues in leaves. Carbendazim may be anticipated to metabolize in the animal into hydroxylated analogues which may appear in meat and milk products. Carbendazim acts as a mitotic poison by altering tubulin binding and microtubule formation. This has been proposed as a possible mechanism of action for the developmental abnormalities seen in animal studies with high concentrations.

Ortataxel (previously known as IDN 5109 or BAY59-8862), a second-generation taxane derivative that was developed as an antitumor agent. Ortataxel binds to and stabilizes tubulin molecules, thereby interfering with the dynamics of microtubule assembly/disassembly. This results in the inhibition of cell division and cellular proliferation. In addition, ortataxel modulates multi-drug resistance mechanisms and may be useful for treating multi-drug resistant tumors that express Pgp, MRP-1, and BCRP. This drug participated in phase II clinical trials in patients with advanced renal cell carcinoma and in patients with Non-Hodgkin's lymphoma. However, these studies were discontinued. Ortataxel was also involved in phase II clinical trials for patients with glioblastoma; however, in a limited number of patients, the drug produced a benefit that lasted for a long time. Besides, ortataxel successfully completed phase II trials in taxane-resistant metastatic breast cancer patients and in taxane-resistant non-small cell lung cancer patients.

Epothilone D (KOS-862 or BMS-241027) is an intermediary obtained in the synthesis of members of the epothilone family and is a small-molecule microtubule stabilizer. It was investigated in Phase II trials in colorectal, metastatic breast and non-small-cell lung cancers. However, development was discontinued in 2007 in favor of a second-generation analog with a better safety profile. This drug also was studied for the treatment of Alzheimer's disease. The study ended in October 2013, and evaluation of epothilone D for Alzheimer's disease was subsequently discontinued. The mechanism by which epothilones induce microtubule polymerization appears to be similar to that of paclitaxel, in that epothilones compete with paclitaxel for binding to microtubules and suppress microtubule dynamics in a manner similar to that of paclitaxel.

Monomethyl Auristatin E (MMAE) is an antimitotic agent which inhibits cell division by blocking the polymerization of tubulin. Monomethyl Auristatin E is the synthetic analog of the antineoplastic natural product Dolastatin 10, cannot be used as a drug itself. Monomethyl Auristatin E is commonly conjugated with monoclonal antibodies directed at antigens specific to cancer cells for tumor-directed cytotoxicity. MMAE is typically coupled to the antibody via a protease-cleavable linker, allowing separation of the drug from the antibody following intracellular localization. When coupled to cAC10, Monomethyl Auristatin E shows selective cytotoxicity in CD30+ cells and induces G2/M-phase growth arrest and cell death through the induction of apoptosis. When coupled to the anti-CD79b antibody, anti–CD79b-vcMMAE has very potent and broad activity across a large panel of NHL cell lines in vitro. When coupled to the anti-HER2 antibody, pertuzumab-vc-MMAE can also be effectively internalized and potently kill HER2 over-expressing tumor cells. In the Karpas 299 ALCL model, cAC10-vcMMAE induces complete, durable tumor regression, while free MMAE doesn’t produce detectable antitumor activity. In mouse xenograft models of NHL, anti–CD79b-vcMMAE strikingly results in sustained complete tumor remission.

Epothilone A is a natural compound, originally discovered from the myxobacterium Sorangium cellulosum. Epothilones A, a macrolide compound, stabilizes polymerized microtubules, leading to mitotic arrest and cytotoxicity in proliferating cells. While epothilone A shows potent antineoplastic activity in vitro, these effects were not seen in preclinical in vivo models due to its poor metabolic stability and unfavorable pharmacokinetics.