Antineoplastons are a mixture of peptides and amino acids present in human blood and urine. These were first isolated from blood and urine by Stanislaw Burzynski. He claims to have utilized antineoplastons to treat various cancers based on the faith that they promote the body’s natural defences against cancer.

According to him, antineoplastons are components of a biochemical surveillance system in the body that work as “molecular switches”. For Burzynski, cell differentiation is the key to cancer therapy. At the molecular level, these abnormal cells that are potential cancer cells need to be “switched” to normal. Antineoplastons are the surveillance system that regulates cancer cells into normal channels of differentiation; as stated by Burzynski, people with cancer are deficient in this surveillance system because they do not have enough antineoplastons.

The idea of controlling tumor growth by a naturally occurring biochemical mechanism in the body that directs these abnormal cancer cells into normal channels of differentiation is one of the theoretical bases of antineoplaston therapy. In the body, cells are continuously differentiating. Groups of abnormal cells can originate under carcinogenic factors from the external or inside the body. The body must have a system for dealing with these abnormal cells, or the organism will not exist very long. The proposed component that sends these abnormal cells to divide normally like healthy cells is ‘antineoplastons’.

Burzynski defines antineoplastons as “substances produced by the living organism that protect them against the origination of neoplastic growth by some non immunological process which does not significantly inhibit the growth of normal tissues”.

Hypothesizing that peptides were the carriers of cell’s differentiation information, the developer began studying for peptides present in the blood of cancer patients that might fix abnormal differentiation.

After the commencement of his research on antineoplastons in human blood and urine, Dr. Burzynski found out that there are two types of antineoplastons;- one with broad-spectrum antineoplastic activity the other with specific antineoplastic activity. The ones with broad-spectrum antineoplastic activity are known as ‘antineoplastons A’, whereas specific antineoplaston activity has not been investigated further.

After the purification of antineoplaston A, it yields fractions of antineoplastons A1, A2, A3, A4, and A5. It is found that each fraction of antineoplastons has higher antitumor activity and low toxicity levels than the antineoplaston A alone.

In Phase 1, trial A2 contributes to the highest tumor response rate. The active compound found in A2 is 3-phenylacetyl amino-2,6-piperinedione, which is called antineoplaston 10. Derivatives of antineoplaston 10 are:-

  • AS2-5- it is phenylacetylglutamine (PAG).
  • AS2-1- it is a 4:1 mixture of phenylacetic acid (PA) and PAG.
  • A5- it is a mixture of PA and aromatic fatty acid.


Inadequate Evidence for

  • Brain tumor. Early research exhibits that using antineoplaston together with standard medications after radiation and cancer surgery might help decrease brain tumors in some people. Other early research shows that jabbing antineoplastons intravenously might help lessen the size of a specific type of brain tumor, called a glioma, in some adults and children. But other research shows that antineoplastons don’t decrease tumor size in people with gliomas. All of the study until the date is low-quality.
  • Colon cancer. Early research shows that jabbing antineoplastons intravenously and then consuming them via oral route might aid people having colon cancer to live longer after having a part of their liver removed.
  • A rare tumor that affects the CNS is a primitive neuroectodermal tumor. By injecting antineoplastons intravenously (by IV) might help decrease the size of PNETs or keep PNETs from becoming bigger in some children with PNET. But, the research to date is low-quality.
  • Prostate cancer. Injecting antineoplastons with the drug diethylstilbestrol might improve the chance of remission in people with cancer. Again, the research to date is low-quality.
  • Lung cancer
  • Liver cancer
  • Breast cancer


  • Brain swelling due to encephalitis.
  • Sickle cell anemia
  • Parkinson disease
  • other conditions.

More evidence is required to check the efficacy of antineoplastons in the above-said conditions.


Suggested mechanisms for the anticancer activity of antineoplastons include activation of the tumor suppressor gene p53 by phenylacetate and AS2-1, metabolites of A10. Phenylacetylglutamine(PAG), the main component of A10-I, may inhibit the uptake of amino acids necessary for cancer cell growth. A10 also inhibits programmed cell death of neutrophils in breast cancer cells. Since depletion of neutrophils is connected with cancer development, researchers suggest a role for A10 as adjuvant therapy for breast cancer. 


Studies have reported the effect of antineoplastons in some types of cancer:

  • The effect of antineoplastons A10 and AS2-1 on brain tumors were analyzed at Dr. Burzynski’s clinic and the Mayo Clinic. A brain tumor research done in Japan did not state the type of antineoplaston used.
  • The effect of antineoplaston AS2-1 on prostate cancer was analyzed at Dr. Burzynski’s clinic.
  • The effect of antineoplaston A10 on liver cancer is considered in a case report from Japan.

These studies reported miscellaneous results, including cancer remissions. Other researchers have not achieved the same results reported by Dr. Burzynski and his team. Some of the patients in the reported studies got standard treatments in addition to the antineoplastons. In these cases, it is unknown if responses and side effects were produced by antineoplaston therapy, the other treatments, or both. One additional independent study from Japan was finished but did not have the same findings as the Burzynski report.

Randomized controlled trials produce the highest level of proof. In these trials, volunteers are put randomly into one of 2 or more groups that compare various treatments. The Control group does not get the new treatment being analyzed. The control group is compared to the groups that get the new treatment to examine if the new treatment works. No randomized, controlled trials depicting the effectiveness of antineoplastons have been published in peer-reviewed scientific journals.

In 1991, the National Cancer Institute analyzed some of Dr. Burzynski’s cases and decided to conduct clinical trials on antineoplastons at cancer centers. By August 1995, only nine subjects had registered, and the clinical trials ended before being completed. Food and Drug Administration of the UK has given Dr. Burzynski approval to conduct clinical trials of antineoplaston therapy at his clinic. Ongoing non-randomized clinical trials at the Burzynski clinic carry on to study the effect of antineoplastons on cancer.

The antineoplastons now utilized in clinical trials are A10, AS2-5, AS2-1, A2, A3, and A5.


Antineoplaston is administered in various ways. Antineoplaston A has been given intravenously, intramuscularly, intrapleural, rectally, topically and by bladder instillation. Antineoplastons such as A10, AS2-5, AS2-1, A2, A3, and A5 are delivered orally or jabbed.

Antineoplastons are possibly safe when used orally and adequately. Oral consumption of Antineoplaston A10 in amounts 8-10g/day for up to 20 days is safe. Antineoplaston AS2-1 may be utilized orally and intravenously, safely, in 12g/day doses for up to 20 days. Infused antineoplaston A10 may be safe in quantities of up to 20g/day for up to 7 days, whereas infused antineoplaston AS2-1 may be safe when delivered in doses up to 10 grams/day for up to 7 days.


The approved dosage for Antineoplastons depends on what it is being used for.

For prostate cancer– the recommended dosage is 97-130 mg per kg of Antineoplaston AS2-1 daily, consuming orally for 64-425 days together with 0.01-0.02 mg per kg diethylstilbestrol every day.

It is advised to take IV injections of 7.7 gram per kg of antineoplaston A10 every day and 0.36 gram per kg of antineoplastons AS2-1 daily for a brain tumor.

It is recommended for patients with recurrent glioma to take IV injections of 1.0-11.3 grams per kg of A10 and 0.4 gram per kg of AS2-1 every day for about 2 to 6 months. For children with repetitive glioma, the recommended dosage is 0.28 gram per kg of antineoplastons A10 daily, and 0.28 gram per kg of AS2-1 delivered orally for 19 months.

For primitive neuroectodermal tumors (PNET), it is prescribed to use IV infusions containing a mixture of antineoplaston A10 and AS2-1 for 1.2 to 67 months. The recommended dose of A10 is 10.3 grams per kg regular, and the recommended amount of AS2-1 is 0.38 grams per kg daily.


Side effects include:-

  • malaise
  • anemia
  • headaches
  • abdominal gas
  • mild myelosuppression
  • nausea and vomiting
  • seizures
  • sleepiness
  • dehydration
  • increased amylase
  • hypokalemia
  • hyperkalemia
  • reduced albumin
  • phlebitis etc.


Because of the lack of adequate information, it is recommended not to use antineoplastons in pregnancy or the lactation period.

Before taking antineoplastons, do consult your doctor.