VAL23 Sep 2020 19:46
VAL 201 is equally efficacious in androgen-AR and estradiol-ER modulation, and this opens up a range of potential disease targets beyond prostate cancer. There is significant potential for the use of VAL 201 as a treatment for other metastatic cancers including breast, endometrial and ovarian cancer, but its development for these indications is at an early stage. Preclinical testing, has demonstrated that VAL 201 inhibits the estradiol-induced association between the ER and Src without interfering in receptor-dependent transcriptional activity in MCF-7 mammary cancer cells.26
Another potential role for VAL 201 in the future is an alternative to chemical or surgical castration in patients with low-risk prostate cancers. Upon diagnosis of low-risk early stage prostate cancer, an ‘active surveillance’ approach is currently adopted due to the risk/benefit considerations of available drugs. Active surveillance refers to a strategy of forgoing immediate treatment after a diagnosis of prostate cancer in favour of regularly scheduled testing and clinical examinations to monitor disease progression. Many patients are unhappy about a perceived lack of treatment after being diagnosed with cancer and forgo active surveillance, opting for surgical or chemical therapies with undesirable side effects. The theoretically favourable safety profile of VAL 201 means that it could potentially be prescribed at this stage to delay disease progression. Because VAL 201 is a novel therapy, there is the potential for combinational activity with other anti-cancer agents. Synergy of the Src inhibitor dasatinib has been demonstrated in non-prostatecancer models for cisplastin, doxorubicin and temozolomide,33–35 and therefore there is potential for VAL 201 to demonstrate combinational activity.
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