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6-TG 6-thioguanine

Synonyms TG 6-TG 6-thioguanine tioguanine Trade name Lanvis Indications Leukemias Category Antimetabolite Antineoplastic Half-life I I hours... [Pg.566]

Thioguanine (6-TG) -purine analogue antimetabolite cell cycle dependent -bone marrow suppression -nausea and vomiting -mucocutaneous effects (mucositis, stomatitis) -rash -hepatotoxicity -hyperuricemia... [Pg.179]

Methotrexate (Rheumatrex Dose Pack, TrexaU) Nelarabine (Arranon) Pemetrexed (Alimta) 6-Thioguanine [6-TG] (Tabloid)... [Pg.38]

The thiopurines 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) are essential components of treatment protocols for childhood acute lymphoblastic leukemia... [Pg.173]

Fig. 1. Outline of treatment strategy applied in the ALL-Berlin-Frankfurt-Munster (BFM) 95 study (1995-2000). Patients were assigned to standard-risk (SR), intermediate-risk (MR) and high-risk (HR) subgroups. Elements containing 6-mercaptopurine (6-MP) or 6-thioguanine (6-TG) are indicated in grey. Abbreviations PRED-GR, prednisone good response PRED-PR, prednisone poor response DEXA, dexamethasone VCR, vincristine DNR, daunorubicin HD-MTX, high-dose methotrexate LD-ARA-C, low-dose cytarabine SCT, stem cell transplantation. Fig. 1. Outline of treatment strategy applied in the ALL-Berlin-Frankfurt-Munster (BFM) 95 study (1995-2000). Patients were assigned to standard-risk (SR), intermediate-risk (MR) and high-risk (HR) subgroups. Elements containing 6-mercaptopurine (6-MP) or 6-thioguanine (6-TG) are indicated in grey. Abbreviations PRED-GR, prednisone good response PRED-PR, prednisone poor response DEXA, dexamethasone VCR, vincristine DNR, daunorubicin HD-MTX, high-dose methotrexate LD-ARA-C, low-dose cytarabine SCT, stem cell transplantation.
The thiopurines 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG) were synthesized by Elion and Hitchings in the 1950s, and they play an important part in treatment protocols for leukemia (61,62,63,64). For no other than historical reasons, 6-MP is used in ALL while 6-TG is mainly used in acute myeloid leukemia (AML) or relapsed ALL. First-line treatment for childhood ALL usually includes several cycles of 6-MP at doses of 50-75 mg/m /d, starting as early as in consolidation/early intensification treatment until up to 36 months after diagnosis (1,2,3). [Pg.176]

Fig. 7.1 Induction of 6-thioguanine resistance by x rays in TK-6 human diploid lymphoblasts. The line shown, fitted by linear regression analysis, has a sl< of 6.0 0.56 TG" cells per 10 Gy (10 rad) (from Grosovsky and Little, 1985). Fig. 7.1 Induction of 6-thioguanine resistance by x rays in TK-6 human diploid lymphoblasts. The line shown, fitted by linear regression analysis, has a sl< of 6.0 0.56 TG" cells per 10 Gy (10 rad) (from Grosovsky and Little, 1985).
Thioguanine (6-TG) also inhibits several enzymes in the de novo purine nucleotide biosynthetic pathway. Various metabolic lesions result, including inhibition of purine nucleotide interconversion decrease in intracellular levels of guanine nucleotides, which leads to inhibition of glycoprotein synthesis interference with the formation of DNA and RNA and incorporation of thiopurine nucleotides into both DNA and RNA. 6-TG has a synergistic action when used together with cytarabine in the treatment of adult acute leukemia. [Pg.1175]

Mercaptopurine and thioguanine are both given orally (Table 55-3) and excreted mainly in the urine. However, 6-MP is converted to an inactive metabolite (6-thiouric acid) by an oxidation catalyzed by xanthine oxidase, whereas 6-TG requires deamination before it is metabolized by this enzyme. This factor is important because the purine analog allopurinol, a potent xanthine oxidase inhibitor, is frequently used with chemotherapy in hematologic cancers to prevent hyperuricemia after tumor cell lysis. It does this by blocking purine oxidation, allowing excretion of cellular purines that are relatively more soluble than uric acid. Nephrotoxicity and acute gout produced by excessive uric acid are thereby prevented. Simultaneous therapy with allopurinol and 6-MP results in excessive toxicity unless the dose of mercaptopurine is reduced to 25% of the usual level. This effect does not occur with 6-TG, which can be used in full doses with allopurinol. [Pg.1292]

The drug 6-mercaptopurine [mer kap toe PYOOR een] (6-MP) is the thiol analog of hypoxanthine. It and thioguanine (6-TG) were the first purine analogs to prove beneficial for treating neoplastic disease. Azathioprine, an immunosuppressant, exerts its effects after conversion to 6-MP. [Pg.391]

FO, which is a Sp2 + Sp2 hybrid, may require frequent recloning Y3 is a rat myeloma, AI2 a human myeloma, the others are from mouse. Drug resistance 8-Ag and 6-Tg 8-azaguanine and 6-thioguanine (cells lack hypoxanthine phosphoribosyl transferase) BUdR S-bromo-2-deoxyuridine (cells lack thymidine kinase). [Pg.66]

See other pages where 6-TG 6-thioguanine is mentioned: [Pg.1302]    [Pg.639]    [Pg.179]    [Pg.1160]    [Pg.144]    [Pg.1017]    [Pg.84]    [Pg.232]    [Pg.1302]    [Pg.639]    [Pg.1160]    [Pg.144]    [Pg.1017]    [Pg.232]    [Pg.147]    [Pg.149]    [Pg.1285]    [Pg.184]    [Pg.68]    [Pg.155]    [Pg.301]    [Pg.178]    [Pg.179]    [Pg.195]    [Pg.1163]    [Pg.153]    [Pg.301]    [Pg.393]    [Pg.147]    [Pg.149]    [Pg.675]    [Pg.167]    [Pg.2300]    [Pg.2325]    [Pg.575]    [Pg.84]   
See also in sourсe #XX -- [ Pg.301 ]

See also in sourсe #XX -- [ Pg.301 ]

See also in sourсe #XX -- [ Pg.301 ]



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6-Thioguanine

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