Otaplimastat is primarily investigated for its potential in cancer therapy, particularly due to its ability to inhibit matrix metalloproteinases (MMPs), especially MMP-13. These enzymes are involved in breaking down the extracellular matrix, a process that facilitates tumor invasion and metastasis. By targeting MMP-13, otaplimastat may help suppress tumor progression and spread in cancers such as osteosarcoma and other solid tumors.

It has shown promise in preclinical studies for reducing cancer cell migration and invasion, making it a candidate for adjuvant therapy in combination with conventional chemotherapy or immunotherapy. Additionally, otaplimastat is being explored for its role in modulating the tumor microenvironment, potentially enhancing the effectiveness of other anticancer agents.

Research is ongoing to evaluate its efficacy and safety in clinical settings, with a focus on cancers where MMP-13 overexpression correlates with poor prognosis.