Pimavanserin tartrate is a potent 5-HT 2A receptor inverse agonist used to treat Parkinson's disease-related psychosis, with the most potent inhibitory activity on the NFAT signaling pathway.

5-HT2A:8.7(pIC50)

METHODS: The pharmacological effects of PVT on TNBC cells were evaluated at specific time points and different concentration ranges (1.25-20 μM). The short-term effects (24-72 hours) of PVT treatment on the proliferation of two TNBC cell lines, 4T1 and MDA-MB-231, were evaluated using MTT assay.
RESULTS The half-maximal inhibitory concentration (IC50) values ​​of PVT on 4T1 cell line at 24 hours, 48 ​​hours and 72 hours were 6.77 μM, 1.94 μM and 1.46 μM, respectively, while the half-maximal inhibitory concentration (IC50) values ​​for MDA-MB-231 were 9.65 μM, 4.24 μM and 2.31 μM, respectively. The inhibitory effect of PVT on the viability of 4T1 and MDA-MB-231 cells showed concentration dependence. However, PVT has a smaller inhibitory effect on the viability of normal human breast epithelial MCF-10A cells.[1]

METHODS: Mice were inoculated with 1 × 105 luciferase-expressing 4T1 cells into the left peritoneal cavity. PVT (30 mg/kg) was administered daily by intraperitoneal injection. When the average tumor volume reached approximately 1000 mm3, the tumors were carefully excised and the wounds sutured. To monitor metastasis, a non-invasive in vivo imaging system was used to detect tumor metastasis. The data were collected and analyzed using Living Image® 4.7.2 software.
RESULTS PVT mildly inhibited the growth of subcutaneous tumors in vivo without causing significant weight loss in the animals. [1]
METHODS: U87 cells were subcutaneously implanted into nude mice to establish a GBM xenograft model. The mice were treated with Pimavanserin tartrate (10 mg/kg, orally, daily, for three weeks), and the tumor growth in the mice was observed.
RESULTS Pimavanserin tartrate significantly inhibited tumor growth. [2]