Drug intelligence / Profile preview

Muscadine Grape Skin Extract

Development stage
Phase 3
Lead developer
Muscadine Naturals
Modality
Small Molecules
Administration
Oral
01

Overview

Muscadine Grape Skin Extract (MPX) is a nutritional supplement derived from the skin of muscadine grapes (Vitis rotundifolia), which are indigenous to the southeastern United States and have been cultivated since the 16th century[2][9]. This extract contains several bioactive compounds including ellagic acid, quercetin, and resveratrol, which have demonstrated antioxidant, anti-inflammatory, and potential anticancer properties[1][2]. ## Composition and Formulation MPX is produced by pulverizing muscadine grape skin, typically from the Noble cultivar of Vitis rotundifolia[3]. Each 500 mg capsule of MPX contains approximately 1.2 mg of ellagic acid, 9.2 μg of quercetin, and 4.4 μg of trans-resveratrol[3]. The extract is manufactured through a process where muscadine grapes are pressed and processed according to good manufacturing practices, then dissolved in water, dried, and converted to powder before being encapsulated in vegetable capsules[6]. ## Mechanisms of Action Several mechanisms have been proposed for MPX's potential anticancer effects: 1. **Antioxidant Activity**: The polyphenols in MPX neutralize free radicals, potentially reducing oxidative stress that contributes to cancer development[9]. 2. **Anti-inflammatory Effects**: MPX has demonstrated anti-inflammatory properties that may help reduce cancer-promoting inflammation[6]. 3. **Cell Cycle Regulation**: Studies show MPX can induce cell-cycle arrest in prostate cancer cells, inhibiting their growth[4]. 4. **Apoptosis Induction**: MPX has been shown to downregulate the PI3K-Akt pathway in prostate cancer cell lines, leading to programmed cell death[9]. 5. **Migration Inhibition**: In metastatic prostate cancer cell lines, MPX inhibited cell migration and invasion, potentially reducing metastatic potential[4][9]. ## Clinical Studies MPX has been investigated in several clinical trials: 1. **Phase I Study in Biochemically Recurrent Prostate Cancer**: This study found that MPX at doses up to 4000 mg daily was safe and well-tolerated with no dose-limiting toxicities. An exploratory review suggested a median 5.3-month lengthening in PSA doubling time (PSADT)[2]. 2. **Phase I Study in Advanced Solid Tumors**: Another phase I study in patients with metastatic and unresectable cancers found that muscadine grape extract was safe and well-tolerated, even among patients with poor performance status[9]. 3. **Phase II Study**: A randomized, multicenter, placebo-controlled phase II trial investigated both low dose (500 mg) and high dose (4,000 mg) MPX in patients with biochemically recurrent prostate cancer[2][3]. ## Commercial Availability MPX is commercially available as a dietary supplement under brand names such as MuscadinePlus and Mighty Muscadine[3][8]. It's important to note that as a dietary supplement, MPX is not regulated as a pharmaceutical drug by the FDA. ## Safety Profile Clinical studies have shown that MPX is generally safe and well-tolerated, even at high doses (up to 1600 mg total phenolics/day)[6]. No dose-limiting toxicities were observed in phase I trials[9]. The extract continues to be investigated for its potential therapeutic applications, particularly in prostate cancer and other advanced solid tumors.

Brand names
MuscadinePlusMighty Muscadine
Other names
muscadine grape extract
02

Targets

Misfolded SOD1

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