Emerging treatments

Tegafur/gimeracil/oteracil

Tegafur/gimeracil/oteracil is an oral fluoropyrimidine. The European Medicines Agency has granted marketing authorisation for tegafur/gimeracil/oteracil as monotherapy or in combination with oxaliplatin or irinotecan, with or without bevacizumab, for the treatment of patients with metastatic colorectal cancer who are unable to continue treatment with another fluoropyrimidine due to hand-foot syndrome or cardiovascular toxicity that developed in the adjuvant or metastatic setting. Tegafur/gimeracil/oteracil is not currently approved in the US. Tegafur is an oral prodrug of fluorouracil, while gimeracil and oteracil are modulators of fluorouracil activity. Gimeracil is a dihydropyrimidine dehydrogenase inhibitor that prevents degradation of fluorouracil, and oteracil is an orotate phosphoribosyltransferase (OPRT) inhibitor that decreases the activity of fluorouracil in normal gastrointestinal mucosa (reducing gastrointestinal toxicity). A phase 3 trial in patients with stage 3 colorectal cancer is ongoing.[363]

Botensilimab plus balstilimab

The FDA has granted fast-track designation to the combination of botensilimab (an investigational monoclonal antibody directed at multi-functional cytotoxic T-lymphocyte-associated protein-4 [CTLA-4]) plus balstilimab (an investigational monoclonal antibody directed at programmed cell death protein-1 [PD-1]) in patients with nonmicrosatellite instability-high/deficient mismatch repair metastatic colorectal cancer with no active liver involvement. In the phase 1B study that was conducted in more than 350 patients, clinical response was observed in nine solid tumour cancers when botensilimab was used alone or in combination with balstilimab. A global, randomised phase 2 trial in nonmicrosatellite instability-high metastatic colorectal cancer is in progress.[364]

Phosphodiesterase-5 inhibitors

Phosphodiesterase-5 inhibitors are being investigated for repurposing for colorectal cancer prevention.[365][366]​​​​[367] In one nationwide population-based study of men with a diagnosis of benign colorectal neoplasm, phosphodiesterase-5 inhibitor use was associated with a greater reduction in advanced-stage colorectal cancer risk than early-stage colorectal cancer risk; however, the difference was not significant.[365] One systematic review and meta-analysis reported that phosphodiesterase-5 inhibitor ever-users had a significantly lower incidence of colorectal cancer than never-users (odds ratio 0.88, 95% confidence interval 0.79 to 0.98, P=0.02).[366] Further studies are warranted to investigate this association.

Transanal total mesorectal excision

Transanal total mesorectal excision (TaTME) is an emerging minimally invasive procedure in which the rectum is dissected transanally according to TME principles. The transanal approach is intended to overcome technical difficulties associated with distal rectal dissection. Long-term, large-scale follow-up data regarding survival, local recurrence, oncological safety, and functional results are awaited; ongoing audit and prospective trials are recommended.[368][369][370]

Radiolabelled microspheres

Hollow spheres filled with yttrium-90 (Y-90) are used in an interventional radiology procedure known as selective internal radiation therapy (SIRT) or radioembolisation. The procedure targets high doses of radiation directly to unresectable liver metastases. Studies in colorectal cancer report mixed results; some demonstrated improved progression-free survival and an overall survival benefit, others demonstrated no improvement in either disease progression or overall survival.[371][372][373][374][375][376]​​ One systematic review comprising 11 retrospective and three prospective studies on Y-90 radioembolisation reported overall survival of about 9 months, suggesting that there was no significant improvement in overall survival over previous studies.[377]​ Combined analysis of three multicentre, randomised, phase 3 trials found that the addition of SIRT to first-line FOLFOX chemotherapy for patients with liver-only and liver-dominant metastatic colorectal cancer did not improve overall survival compared with that for FOLFOX alone.[378]​ The study concluded that, to further define the role of SIRT in metastatic colorectal cancer, careful patient selection and studies investigating the role of SIRT as consolidation therapy after chemotherapy are needed.

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