One of the most challenging situations any integrative doctor like myself faces is when a cancer patient with late-stage-4 disease presents to the office for the first time having failed all previous treatments, is cachectic and in constant pain, is experiencing persistent nausea and vomiting that prevents them from taking few, if any, supplements or repurposed medications, is anxious or depressed, and is unable to travel to receive regular intravenous treatments, and yet, amazingly, still has the will to live. Given such circumstances, how does one begin to come up with treatment options and try to turn the disease around? There may be an answer…
A phenomenon present in nearly all cancers is the overexpression of Neurokinin-1 receptor (NK-1r)—a type of protein that is involved in the signaling pathways of substance P (SP), a neuropeptide that plays a central role in cancer, including the regulation of cancer stem cells. The activation of NK-1r by SP has been shown to be a key player in the regulation of cancer cell proliferation, migration, and survival, as well as holding a vital function in regulating the self-renewal and tumor-forming potential of cancer stem cells. Here is a list of known cancers that express NK-1r:
- Astrocytoma
- Breast
- Cervical
- Colon
- Endometrial
- Esophageal
- Gastric
- Glioblastoma multiforme
- Hepatocellular carcinoma
- Laryngeal
- Leukemia
- Lung
- Melanoma
- Neuroblastoma
- Osteosarcoma
- Ovarian
- Pancreatic
- Prostate
- Retinoblastoma
- Thyroid
According to scientists, a drug that can safely block NK-1r (and thus block SP) would be a “broad spectrum anti-tumor drug” by possessing multiple actions against cancer as a single agent and might be considered “an intelligent bullet against cancer.” Such a drug may have been found, and that drug is aprepitant (Emend). Aprepitant is a medication that was FDA-approved in 2003 to help prevent nausea and vomiting caused by chemotherapy or surgery. For chemotherapy-induced nausea and vomiting, aprepitant is typically given as a single dose of 125 mg orally on the first day of chemotherapy, followed by 80 mg orally once daily for the next two days. For postoperative nausea and vomiting, aprepitant is usually given as a single dose of 80 mg taken on the evening before surgery.
Being an antiemetic (anti-nausea) drug, aprepitant can decrease nausea and vomiting so that the challenging patient described above can begin to eat again and gain much-needed weight, and tolerate taking supplements and medications. If further appetite stimulation is needed, megestrol acetate can be added, and now with a higher degree of safety as aprepitant has been found to decrease the risk of thrombosis and thromboembolism in cancer patients (there is a risk of blood clots associated with the use of megestrol acetate). Furthermore, aprepitant has been found to exert antianxiety, antidepressant, and analgesic (pain-relieving) actions.
In conclusion, treating a late-stage-4 cancer patient who has failed all previous treatment efforts and is facing multiple physical and emotional challenges can be a daunting task for any integrative cancer doctor. However, new research has shed light on the potential use of aprepitant as a broad-spectrum anti-tumor drug that can target the overexpression of the Neurokinin-1 receptor (NK-1r). By blocking the activation of NK-1r and substance P (SP), aprepitant as a single agent may inhibit cancer cell proliferation, migration, and survival of cancer cells and cancer stem cells. With higher and chronic dosing, aprepitant has the potential to provide not only antiemetic benefits but also antianxiety, antidepressant, and analgesic actions, allowing patients to regain the ability to fight their cancer.
Note: Reprofiling aprepitant as a potential broad-spectrum antitumor agent requires much higher dosing and over a longer period of time: >20 mg/kg/day. For a 70 kg individual, this would equate to around 1500 mg per day. Insurance and Medicare will not cover the high cost of this non-standard dosage. Even using a discount coupon from GoodRx.com, the lowest monthly price of aprepitant is over $13,000 (click here). To significantly reduce the cost for our patients, we get pharmaceutical-grade aprepitant powder custom-synthesized by medicinal chemists at a fraction of the cost of aprepitant capsules at the local pharmacy. We then make it into an oral liposomal solution to increase bioavailability. The cost to our patients is $1,250 for a month’s supply of the medication (vs. $13,000).
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