Sivifene (INN, USAN; developmental code name A-007) is a small-molecule antineoplastic agent and immunomodulator that was under development in the 2000s by Tigris Pharmaceuticals (now Kirax Corporation) as a topical treatment for cutaneous cancer metastases.[1][2][3] It was specifically being investigated to treat high-grade squamous intraepithelial lesions (HSIL) associated with human papillomavirus (HPV) infection and invasive carcinomas of the anogenital area such as cervical, vaginal, and anal cancers.[1] The drug reached phase II clinical trials prior to its discontinuation.[1]
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| Other names | A-007; 4,4'-Dihydroxybenzophenone-2,4-dinitrophenylhydrazone |
| Routes of administration | Topical |
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| Formula | C19H14N4O6 |
| Molar mass | 394.343 g·mol−1 |
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Initially, due to its structural similarity to tamoxifen, sivifene was thought to be a selective estrogen receptor modulator (SERM), but subsequent research revealed that it does not bind to the estrogen receptor (ER) and does not possess antiestrogenic activity.[2] The actual mechanism of action of sivifene is unknown, but it is thought to produce its immunomodulating effects via upregulation of the CD45 T-lymphocyte cell surface receptor.[2]
See also edit
References edit
- ^ a b c "Sivifene - AdisInsight".
- ^ a b c Eilender D, LoRusso P, Thomas L, McCormick C, Rodgers AH, Hooper CL, Tornyos K, Krementz ET, Parker S, Morgan LR (2006). "4,4'-Dihydroxybenzophenone-2,4-dinitrophenylhydrazone (A-007): a topical treatment for cutaneous metastases from malignant cancers". Cancer Chemother. Pharmacol. 57 (6): 719–26. doi:10.1007/s00280-005-0124-2. PMID 16184382. S2CID 10830366.
- ^ Robert A. Schwartz (30 April 2008). Skin Cancer: Recognition and Management. John Wiley & Sons. pp. 267–. ISBN 978-0-470-69563-0.