Clinical trial risk in castration-resistant prostate cancer: immunotherapies show promise was written by Tenuta, Alessandro;Klotz, Laurence;Parker, Jayson L.. And the article was included in BJU International in 2014.Formula: C20H15ClN4 This article mentions the following:
The objectives of the study were to determine the risk of failure during drug development in castration-resistant prostate cancer (CRPC) and to identify factors that could improve outcomes. We investigated CRPC by analyzing compounds in phase I to phase III clin. trials between 1998 and Apr. 2011. Drug development failures were classified as medical or com. and were compared with industry expectations. Compounds were excluded from anal. if their phase I occurred before 1998, if they targeted patients that were did not have hormone-refractory prostate cancer, or if they did not assess outcomes such as overall survival, time to disease progression, or prostate-specific antigen levels. Thorough searches of clinicaltrial.gov and other databases yielded 77 compounds that met the inclusion criteria. The cumulative pass rate for first-line compounds in CRPC was 3% and was far below aggregate industry expectations. In total, there were nearly equivalent numbers of com. and medical failures. Biol. products were found to have had greater relative success than small-mol. drugs and biotechnol. firms had been slightly more successful than pharmaceutical firms in this disease indication. Phase III failures were high, despite equally high failures during phase II. Currently, one in 33 compounds that enters clin. testing will be awarded US Food and Drug Administration approval. This appears to be the highest risk indication investigated to date, based on clin. trial studies alone, with an average cost of 1.411bn to bring a new drug to market when adjusted for risk. Development of radical therapeutics such as immunotherapies may also be warranted instead of classic antineoplastic therapeutics. Given the high clin. trial risk, efforts may have to shift to biomarker and surrogate endpoints to manage future clin. trial risk in prostate cancer. In the experiment, the researchers used many compounds, for example, N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3Formula: C20H15ClN4).
N-(4-Chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine (cas: 212141-54-3) belongs to phthalazine derivatives. Phthalazines, as an important class of bicyclic N-heterocycles, have attracted sizable attention due to their valuable biological and pharmacological activities. Phthalazine derivatives are also considered as p38MAP kinase inhibitors, selective binders of gamma-aminobutyric acid (GABA) receptors, cyclooxygenase-2 (COX-2) inhibitors, and high-affinity ligands of voltages gated calcium channels.Formula: C20H15ClN4
Referemce:
Phthalazine – Wikipedia,
Phthalazine | C8H6N2 – PubChem