3-Phenylacetylamino-2,6-piperidinedione, Antineoplaston A, Antineoplaston A1, Antineoplaston A10, Antineoplaston A10-1, Antineoplaston A2, Antineoplaston A3, Antineoplaston A4, Antineoplaston A5, Antineoplaston AS2-1, Antineoplaston AS2-5, Antineoplaston AS5, Antineoplaston Ch, Antineoplaston F, Antineoplaston H, Antineoplaston K, Antineoplaston L, Antineoplaston O, Phenylacetate, Phenylacetylglutamine, Phenylacetylisoglutamine.
Antineoplastons are peptides found in the urine and blood of healthy people. The chemical structures of antineoplastons were determined in the 1980s. Today, most antineoplastons are prepared in a laboratory.
Antineoplastons are taken by mouth or injected into veins or muscles for various cancers, including bladder cancer, brain cancer, breast cancer, colon and rectal cancer, liver cancer, and lung cancer.
Antineoplastons are also taken by mouth for high cholesterol, brain swelling due to infection (encephalitis), less advanced cases of HIV/AIDS, Parkinson's disease, sickle cell anemia, and an inherited blood disorder called thalassemia.
Antineoplastons are also injected intravenously (by IV) for advanced cases of HIV/AIDS, excess ammonia in the blood (hyperammonemia), and high cholesterol.
How does work?
Antineoplastons might stimulate the immune system. These peptides might also kill certain cancer cells or prevent them from growing.
Insufficient Evidence to Rate Effectiveness for...
- Brain tumor. Using antineoplastons along with remission therapy following radiotherapy and surgical removal of brain tumors might help reduce tumor size in some people. However, the research to date is low-quality.
- A type of brain tumor called glioma. Injecting two antineoplastons (A10 and AS2-1) intravenously (by IV) might help eliminate or reduce the size of certain brain tumors, called gliomas, in some adults. Also, injecting these antineoplastons by IV then taking these antineoplastons by mouth might help eliminate or reduce the size of these tumors in some children with recurrent gliomas. However, other research shows that antineoplastons A10 and AS2-1 don't reduce tumor size in people with gliomas. All of the research to date is low-quality.
- A type of cancer, called primitive neuroectodermal tumors (PNETs), which affects the central nervous system. Injecting antineoplastons A10 and AS2-1 intravenously (by IV) might help reduce the size of PNETs or prevent the condition from advancing in some children at risk for PNET recurrence. However, the research to date is low-quality.
- Prostate cancer. Injecting antineoplaston AS2-1 along with the drug diethylstilbestrol might increase the chance of remission in people with prostate cancer. However, the research to date is low-quality.
- Breast cancer.
- Colon and rectal cancer.
- Liver cancer.
- Lung cancer.
- High cholesterol.
- Brain swelling due to infection (encephalitis).
- HIV/AIDS.
- Parkinson's disease.
- Sickle cell anemia.
- An inherited blood disorder called thalassemia.
- Other conditions.
QUESTION
See AnswerAntineoplastons A10 and AS2-1 are POSSIBLY SAFE when taken by mouth or injected intravenously (by IV) in appropriate amounts for a short time. There is not enough information to know if other forms of antineoplastons are safe when given by mouth or by IV short-term.
Antineoplastons A10 and AS2-1 are POSSIBLY UNSAFE when taken by mouth or injected by IV in higher doses or for longer periods of time. Giving antineoplastons in higher doses or for longer periods of time seems to increase the number of side effects.
Side effects of antineoplastons include irregular heartbeat, increased blood pressure, skin rash, nausea, vomiting, stomach pain, gas, liver problems, joint swelling, muscle and joint pain, weakness, tiredness, headache, ringing in the ears, dizziness, and fever.
Pregnancy and breast-feeding: Not enough is known about the safety of using antineoplastons when pregnant or breast-feeding. It's best to avoid using it.The appropriate dose of antineoplastons depends on several factors such as the user's age, health, and several other conditions. At this time, there is not enough scientific information to determine an appropriate range of doses for antineoplastons. Keep in mind that natural products are not always necessarily safe and dosages can be important. Be sure to follow relevant directions on product labels and consult your pharmacist or physician or other healthcare professional before using.
Natural Medicines Comprehensive Database rates effectiveness based on scientific evidence according to the following scale: Effective, Likely Effective, Possibly Effective, Possibly Ineffective, Likely Ineffective, and Insufficient Evidence to Rate (detailed description of each of the ratings).
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Abou-Zeid LA, El Mowafy AM, el Ashmawy MB, et al. Novel piperidinedione analogs as inhibitors of breast cancer cell growth. Arch Pharm (Weinheim) 2000;333(12):431-434. View abstract.
Ashraf AQ, Liau MC, Kampalath BN, Burzynski SR. Pharmacokinetic study of radioactive antineoplaston A10 following oral administration in rats. Drugs Exp Clin Res 1987;13 Suppl 1:45-50. View abstract.
Ashraf AQ, Liau MC, Mohabbat MO, Burzynski SR. Preclinical studies on antineoplaston A10 injections. Drugs Exp Clin Res 1986;12 Suppl 1:37-45. View abstract.
Badria F, Mabed M, El Awadi M, et al. Immune modulatory potentials of antineoplaston A-10 in breast cancer patients. Cancer Lett 2000;157(1):57-63. View abstract.
Buckner JC, Malkin MG, Reed E, et al. Phase II study of antineoplastons A10 (NSC 648539) and AS2-1 (NSC 620261) in patients with recurrent glioma. Mayo Clin Proc 1999;74(2):137-145. View abstract.
Burstein AH, Reed E, Tompkins AC, Venzon D, Figg WD. Phenylacetate pharmacokinetics based on iterative two-stage population analysis. Pharmacotherapy 2001;21(3):281-286. View abstract.
Burzynski SR, Burzynski B, Mohabbat MO. Toxicology studies on antineoplaston AS2-1 injections in cancer patients. Drugs Exp Clin Res 1986;12 Suppl 1:25-35. View abstract.
Burzynski SR, Conde AB, Peters A, et al. A retrospective study of antineoplastons A10 and AS2-1 in primary brain tumors. Clin Drug Invest 1999;18(1):1-10.
Burzynski SR, Kubove E, Burzynski B. Phase I clinical studies of antineoplaston A5 injections. Drugs Exp Clin Res 1987;13 Suppl 1:37-43. View abstract.
Burzynski SR, Kubove E, Burzynski B. Phase I clinical studies of antineoplaston A5 injections. Drugs Exp Clin Res 1987;13 Suppl 1:37-43. View abstract.
Burzynski SR, Kubove E, Burzynski B. Treatment of hormonally refractory cancer of the prostate with antineoplaston AS2-1. Drugs Exp Clin Res 1990;16(7):361-369. View abstract.
Burzynski SR, Kubove E. Initial clinical study with antineoplaston A2 injections in cancer patients with five years' follow-up. Drugs Exp Clin Res 1987;13 Suppl 1:1-11. View abstract.
Burzynski SR, Kubove E. Phase I clinical studies of antineoplaston A3 injections. Drugs Exp Clin Res 1987;13 Suppl 1:17-29. View abstract.
Burzynski SR, Kubove E. Toxicology studies on antineoplaston A10 injections in cancer patients. Drugs Exp Clin Res 1986;12 Suppl 1:47-55. View abstract.
Burzynski SR, Lewy RI, Weaver R, et al. Long-term survival and complete response of a patient with recurrent diffuse intrinsic brain stem glioblastoma multiforme. Integr Cancer Ther 2004;3(3):257-261. View abstract.
Burzynski SR, Lewy RI, Weaver RA, et al. Phase II study of antineoplaston A10 and AS2-1 in patients with recurrent diffuse intrinsic brain stem glioma: a preliminary report. Drugs R D 2003;4(2):91-101. View abstract.
Burzynski SR, Mohabbat MO, Burzynski B. Human toxicology studies on oral formulation of Antineoplaston A10. Drugs Exp Clin Res 1984;10(12):891-909.
Burzynski SR, Mohabbat MO, Lee SS. Preclinical studies on antineoplaston AS2-1 and antineoplaston AS2-5. Drugs Exp Clin Res 1986;12 Suppl 1:11-16. View abstract.
Burzynski SR, Mohabbat MO. Chronic animal toxicity studies on antineoplaston A2. Drugs Exp Clin Res 1986;12 Suppl 1:73-75. View abstract.
Burzynski SR, Stolzmann Z, Szopa B, Stolzmann E, Kaltenberg OP. Antineoplaston A in cancer therapy. (I). Physiol Chem Phys 1977;9(6):485-500. View abstract.
Burzynski SR, Weaver RA, Janicki T, et al. Long-term survival of high-risk pediatric patients with primitive neuroectodermal tumors treated with antineoplastons A10 and AS2-1. Integr Cancer Ther 2005;4(2):168-177. View abstract.
Burzynski SR, Weaver RA, Lewy RI, et al. Phase II study of antineoplaston A10 and AS2-1 in children with recurrent and progressive multicentric glioma : a preliminary report. Drugs R D 2004;5(6):315-326. View abstract.
Burzynski SR. Antineoplastons: history of the research (I). Drugs Exp Clin Res 1986;12 Suppl 1:1-9. View abstract.
Burzynski SR. Potential of antineoplastons in diseases of old age. Drugs Aging 1995;7(3):157-167. View abstract.
Burzynski SR. The present state of antineoplaston research (1). Integr Cancer Ther 2004;3(1):47-58. View abstract.
Burzynski SR. Toxicology studies on antineoplaston AS2-5 injections in cancer patients. Drugs Exp Clin Res 1986;12 Suppl 1:17-24. View abstract.
Ferrandina G, Melichar B, Loercher A, et al. Growth inhibitory effects of sodium phenylacetate (NSC 3039) on ovarian carcinoma cells in vitro. Cancer Res 1997;57(19):4309-4315. View abstract.
Hashimoto K, Koga T, Shintomi Y, et al. The anticancer effect of antineoplaston A-10 on human breast cancer serially transplanted to athymic mice. Nippon Gan Chiryo Gakkai Shi 1990;25(1):1-5. View abstract.
Juszkiewicz M, Chodkowska A, Burzynski SR, et al. The influence of antineoplaston A5 on the central dopaminergic structures. Drugs Exp Clin Res 1994;20(4):161-167. View abstract.
Juszkiewicz M, Chodkowska A, Burzynski SR, Mlynarczyk M, Kleinrok Z. The influence of antineoplaston A5 on particular subtypes of central dopaminergic receptors. Drugs Exp Clin Res 1995;21(4):153-156. View abstract.
Kampalath BN, Liau MC, Burzynski B, Burzynski SR. Chemoprevention by antineoplaston A10 of benzo(a)pyrene-induced pulmonary neoplasia. Drugs Exp Clin Res 1987;13 Suppl 1:51-55. View abstract.
Kumabe T, Tsuda H, Uchida M, et al. Antineoplaston treatment for advanced hepatocellular carcinoma. Oncol Rep 1998;5(6):1363-1367. View abstract.
Lee SS, Burzynski SR. Inducibility of HL-60 leukemic cells to undergo terminal differentiation after repeated treatment with Antineoplaston A5. Int J Exp Clin Chemoth 1990;3(3):125-128.
Lee SS, Burzynski SR. Tissue culture and animal toxicity studies of antineoplaston A5. Drugs Exp Clin Res 1987;13 Suppl 1:31-35. View abstract.
Lee SS, Mohabbat MO, Burzynski SR. In vitro cancer growth inhibition and animal toxicity studies of antineoplaston A3. Drugs Exp Clin Res 1987;13 Suppl 1:13-16. View abstract.
Lee SS, Mohabbat MO, Burzynski SR. Tissue culture and acute animal toxicity studies of antineoplaston A2. Drugs Exp Clin Res 1984;10(8-9):607-610.
Liau M, Liau C, Burzynsky S. Potential of induced terminal differentiation by phenylacetic acid and related chemicals. Int J Exp Clin Chemoth 1992;5:9-17.
Liau MC, Luong Y, Liau CP, et al. Prevention of drug induced DNA hypermethylation by antineoplaston components. Int J Exp Clin Chemoth 1992;5(1):19-27.
Liau MC, Szopa M, Burzynski B, Burzynski SR. Chemo-surveillance: a novel concept of the natural defence mechanism against cancer. Drugs Exp Clin Res 1987;13 Suppl 1:71-76. View abstract.
Liau MC, Szopa M, Burzynski B, Burzynski SR. Quantitative assay of plasma and urinary peptides as an aid for the evaluation of cancer patients undergoing antineoplaston therapy. Drugs Exp Clin Res 1987;13 Suppl 1:61-70. View abstract.
Matono K, Ogata Y, Tsuda H, Araki Y, Shirouzu K. Effects of antineoplaston AS2-1 against post-operative lung metastasis in orthotopically implanted colon cancer in nude rat. Oncol Rep 2005;13(3):389-395. View abstract.
Michalska D. Theoretical investigations on the structure and potential binding sites of antineoplaston A10 and experimental findings. Drugs Exp Clin Res 1990;16(7):343-349. View abstract.
Muldoon TG, Copland JA, Lehner AF, Hendry LB. Inhibition of spontaneous mouse mammary tumour development by antineoplaston A10. Drugs Exp Clin Res 1987;13 Suppl 1:83-88. View abstract.
Nishiguchi Y, Adachi T, Nakazawa M, et al. [A 13-week oral repeated dose toxicity study of (+/-)-4-diethylamino-1,1-dimethylbut-2-yn-1-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate monohydrochloride monohydrate (NS-21), a novel drug for urinary frequency and incontinence, in rats followed by a 5-week recovery test]. J Toxicol Sci 1997;22 Suppl 1:27-57. View abstract.
Oh I, Lee J, Lee Y, Shin S, Choi B. Stability of antineoplaston A10 in aqueous solution. Arch Pharm Res 1995;18:75-78.
Okasaki K, Baba S, Ikeda H, et al. [A 26-week oral repeated dose toxicity study of (+/-)-4-diethylamino-1,1-dimethylbut-2-yn-1-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate monohydrochloride monohydrate (NS-21), a novel drug for urinary frequency and incontinence, in rats followed by a 9-week recovery test]. J Toxicol Sci 1997;22 Suppl 1:59-92. View abstract.
Onishi T, Yamakawa K, Franco OE, Suzuki R, Kawamura J. p27Kip1 is the key mediator of phenylacetate induced cell cycle arrest in human prostate cancer cells. Anticancer Res 2000;20(5A):3075-3081. View abstract.
Potempska A, Loo YH, Wisniewski HM. On the possible mechanism of phenylacetate neurotoxicity: inhibition of choline acetyltransferase by phenylacetyl-CoA. J Neurochem 1984;42:1499-1501. View abstract.
Revelle LK, D'Avignon DA, Wilson JA. 3-[(Phenylacetyl)amino]-2,6-piperidinedione hydrolysis studies with improved synthesis and characterization of hydrolysates. J Pharm Sci 1996;85(10):1049-1052. View abstract.
Samid D, Shack S, Sherman LT. Phenylacetate: a novel nontoxic inducer of tumor cell differentiation. Cancer Res 1992;52(7):1988-1992. View abstract.
Schardein JL, York RG, Ninomiya H, Watanabe M, Sumi N. [Reproductive and developmental toxicity studies of (+/-)-4-diethylamino-1,1-dimethylbut-2-yn-1-yl 2-cyclohexyl-2-hydroxy-2-phenylacetate monohydrochloride monohydrate(NS-21), a novel drug for urinary frequency and incontinence (4). Perinatal and postnatal study in rats by oral administration]. J Toxicol Sci 1997;22 Suppl 1:239-249. View abstract.
Soltysiak-Pawluczuk D, Burzynski SR. Cellular accumulation of antineoplaston AS21 in human hepatoma cells. Cancer Lett 1995;88(1):107-112. View abstract.
Sugita Y, Tsuda H, Maruiwa H, et al. The effect of antineoplaston, a new antitumor agent on malignant brain tumors. Kurume Med J 1995;42(3):133-140. View abstract.
Thibault A, Cooper MR, Figg WD, et al. A phase I and pharmacokinetic study of intravenous phenylacetate in patients with cancer. Cancer Res 1994;54(7):1690-1694. View abstract.
Tsuda H, Hara H, Eriguchi N, et al. Toxicological study on antineoplastons A-10 and AS2-1 in cancer patients. Kurume Med J 1995;42(4):241-249. View abstract.
Tsuda H, Iemura A, Sata M, et al. Inhibitory effect of antineoplaston A10 and AS2-1 on human hepatocellular carcinoma. Kurume Med J 1996;43(2):137-147. View abstract.
Vasse M, Thibout D, Paysant J, et al. Decrease of breast cancer cell invasiveness by sodium phenylacetate (NaPa) is associated with an increased expression of adhesive molecules. Br J Cancer 2001;84(6):802-807. View abstract.
Wang H, Xu W, Yuan Y. Studies of the release rate and bioavailability of antineoplaston A10 capsule. Drugs Exp Clin Res 1990;16(7):357-359. View abstract.
Watanabe M, Sugano S, Imai J, et al. Suppression of tumourigenicity, and induction of differentiation of the canine mammary tumour cell line MCM-B2 by sodium phenylacetate. Res Vet Sci 2001;70(1):27-32. View abstract.
Wood CG, Lee C, Grayhack JT, et al. Phenylacetate and phenylbutyrate promote cellular differentiation in human prostate cancer systems (Meeting abstract). Proc Annu Meet Am Assoc Cancer Res 1994;35:A2404.
Xu W, Wang H, Yuan Y. Pharmacokinetic study of radioactive antineoplaston A10 in rats and mice. Drugs Exp Clin Res 1990;16(7):351-5. View abstract.