TOL-463

TOL-463 is an anti-infective medication which is under development for the treatment of bacterial vaginosis (BV) and vulvovaginal candidiasis (VVC) (vaginal yeast infection).[3][1][4][2] It is a boric acid-based vaginal anti-infective enhanced with ethylenediaminetetraacetic acid (EDTA) which was designed to have improved activity against vaginal bacterial and fungal biofilms while sparing protective lactobacilli.[1][2][4] EDTA enhances the antimicrobial activity of boric acid and improves its efficacy against relevant biofilms.[1] In a small phase 2 randomized controlled trial, TOL-463 as an insert or gel achieved clinical cure rates of 50–59% against BV and 81–92% against VVC in women who had one or both conditions.[4][2][1] It was effective and safe in the study, though it was without indication of superiority over other antifungal medications for VVC.[2][1] The cure rates against BV with TOL-463 were said to be comparable to those with recently approved antibiotic treatments like single-dose oral secnidazole (58%) and single-dose metronidazole vaginal gel (41%).[1] As of May 2019, TOL-463 is in phase 2 clinical trials for the treatment of BV and VVC.[3] It was originated by Toltec Pharmaceuticals and is under development by Toltec Pharmaceuticals and the National Institute of Allergy and Infectious Diseases.[3]

TOL-463
Boric acid (top) and EDTA (bottom)
Combination of
Boric acidAntiseptic, antifungal
EDTAAntimicrobial enhancer
Clinical data
Other namesBoric acid/ethylenediamine-tetraacetic acid; Boric acid/EDTA
Routes of
administration		Vaginal (insert, gel)[1][2]

References
  1. Marrazzo JM, Dombrowski JC, Wierzbicki MR, Perlowski C, Pontius A, Dithmer D, Schwebke J (February 2019). "Safety and Efficacy of a Novel Vaginal Anti-infective, TOL-463, in the Treatment of Bacterial Vaginosis and Vulvovaginal Candidiasis: A Randomized, Single-blind, Phase 2, Controlled Trial". Clin Infect Dis. 68 (5): 803–809. doi:10.1093/cid/ciy554. PMC 6376090. PMID 30184181.
  2. Nyirjesy P, Brookhart C, Lazenby G, Schwebke J, Sobel JD (April 2022). "Vulvovaginal Candidiasis: A Review of the Evidence for the 2021 Centers for Disease Control and Prevention of Sexually Transmitted Infections Treatment Guidelines". Clin Infect Dis. 74 (Suppl_2): S162–S168. doi:10.1093/cid/ciab1057. PMID 35416967.
  3. "TOL 463 - AdisInsight".
  4. Sobel JD, Sobel R (August 2021). "Current and emerging pharmacotherapy for recurrent bacterial vaginosis". Expert Opin Pharmacother. 22 (12): 1593–1600. doi:10.1080/14656566.2021.1904890. PMID 33750246. S2CID 232325625.


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