Systematic Review of Gossypol/at-101 in Cancer Clinical Trials

2022
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15
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Pharmaceuticals 
2022
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15
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22 of 34 
of Medical Sciences) [54,93,94]. AT-101 (NSC# 726190) was supplied by the National 
Cancer Institute Cancer Therapy Evaluation Program as tablets containing 10 mg of the 
drug [88,90,91,96], or as 10 mg immediate release tablets (Ascenta Therapeutics, Inc.) 
taken at the same time each day [92,100], or as 20 mg gossypol acetate tablets produced 
by Xi’an Northern Pharmaceutical Co., Ltd.) [96]. If it was mentioned in the treatment 
plan, gossypol/AT-101 formulation was administered at least 1 h prior to or 1 h after meals 
[92,93,99,100] and prior to i.v. administration [88]. The solubility of poorly soluble active 
agents depends, among other things, on the particle size and the particle wettability. Since 
gossypol is almost insoluble in water, one possibility to increase the solubility of the 
gossypol preparation is micronization, even though this information is not included in the 
studies reviewed. The phrase “immediate release tablet” [92,100] might suggest this and 
would be consistent with the data from Yang et al. [108]. Regarding registered clinical 
trials available on the ClinicalTrials.gov home page, there are no upcoming or active 
interventional trials utilizing gossypol/AT-101 in cancer patients. 
From 17 clinical studies investigating the therapeutic potential of gossypol/AT-101 in 
oncologic patients, there is one trial demonstrating a significant benefit regarding RR or 
SD, or prolongation of survival [95] (Figure 4). 
Figure 4. 
Graphical representation of the results of reviewed studies in cancer clinical trials 
analyzing the administration of gossypol/AT-101 as a single agent or in combination with standard 
anticancer treatments. The pie chart is stratified according to study design (