beta-2--deoxythioguanosine and Neoplasms

beta-2--deoxythioguanosine has been researched along with Neoplasms* in 2 studies

Other Studies

2 other study(ies) available for beta-2--deoxythioguanosine and Neoplasms

Article	Year
Pharmacokinetics and metabolism of beta-2'-deoxythioguanosine and 6-thioguanine in man. Cancer chemotherapy and pharmacology, 1982, Volume: 8, Issue:1 Resistance to the antileukemic agent 6-thioguanine (TG) inevitably develops in animal tumors. However, a new agent, beta-2'-deoxythioguanosine (beta-TGdR) can overcome TG resistance in animal tumor models and is therefore of potential clinical use. The pharmacokinetics of radiolabeled TG were compared with those of beta-TGdR in patients with cancer after intravenous administration. [35S]-beta-TGdR (5.4 mg/kg, 200 mg/m2, 200 microCi total) was administered to five patients; the radiolabel in the plasma declined with an initial half-life (t1/2) of 14 min and a terminal t1/2 of 19.3 h. Within 24 h, 65% of the radiolabel was excreted in the urine. In contrast, after administration of [35S]-6-TG (3.4 mg/kg, 125 mg/m2, 200 microCi total) the average initial t1/2 was 40 min while the terminal phase t1/2 was 28.9 h. Urinary excretion of the radiolabel was 75% of the dose 24 h after administration. Both thiopurines were rapidly and extensively degraded and excreted as 6-thioxanthine, inorganic sulfate, S-methyl-6-thioxanthine, and 6-thiouric acid in addition to other products. Small amounts of unchanged drug were also excreted. These studies suggest that beta-TGdR is merely a latent form of TG. Topics: Allopurinol; Antineoplastic Agents; Deoxyguanosine; Drug Interactions; Humans; Kinetics; Neoplasms; Thioguanine; Thionucleosides	1982
Clinical studies of beta-thioguanine deoxyriboside alone and in combination with arabinosyl cytosine. Medical and pediatric oncology, 1976, Volume: 2, Issue:2 Beta-thioguanine deoxyriboside (betaTGdR) is a purine nucleoside derivative which was studied alone or in combination with arabinosyl cytosine (Ara-C) in patients with solid tumors and acute leukemia. No significant responses were observed in 22 patients with solid tumors. The response rate with betaTGdR alone in acute leukemia was 26% and in combination with Ara-C was 24%. Responses were generally of short duration. Toxicity included myelosuppression, nausea, stomatitis, hyperpigmentation, photosensitivity, and liver function abnormalities. Topics: Acute Disease; Adolescent; Adult; Aged; Child; Child, Preschool; Cytarabine; Deoxyguanosine; Deoxyribonucleosides; Drug Therapy, Combination; Female; Guanosine; Humans; Leukemia; Leukopenia; Male; Middle Aged; Neoplasm Metastasis; Neoplasms; Remission, Spontaneous; Thioguanine; Thionucleosides; Thrombocytopenia; Time Factors	1976

Article

Year

Pharmacokinetics and metabolism of beta-2'-deoxythioguanosine and 6-thioguanine in man.

Cancer chemotherapy and pharmacology, 1982, Volume: 8, Issue:1

Resistance to the antileukemic agent 6-thioguanine (TG) inevitably develops in animal tumors. However, a new agent, beta-2'-deoxythioguanosine (beta-TGdR) can overcome TG resistance in animal tumor models and is therefore of potential clinical use. The pharmacokinetics of radiolabeled TG were compared with those of beta-TGdR in patients with cancer after intravenous administration. [35S]-beta-TGdR (5.4 mg/kg, 200 mg/m2, 200 microCi total) was administered to five patients; the radiolabel in the plasma declined with an initial half-life (t1/2) of 14 min and a terminal t1/2 of 19.3 h. Within 24 h, 65% of the radiolabel was excreted in the urine. In contrast, after administration of [35S]-6-TG (3.4 mg/kg, 125 mg/m2, 200 microCi total) the average initial t1/2 was 40 min while the terminal phase t1/2 was 28.9 h. Urinary excretion of the radiolabel was 75% of the dose 24 h after administration. Both thiopurines were rapidly and extensively degraded and excreted as 6-thioxanthine, inorganic sulfate, S-methyl-6-thioxanthine, and 6-thiouric acid in addition to other products. Small amounts of unchanged drug were also excreted. These studies suggest that beta-TGdR is merely a latent form of TG.

Topics: Allopurinol; Antineoplastic Agents; Deoxyguanosine; Drug Interactions; Humans; Kinetics; Neoplasms; Thioguanine; Thionucleosides

1982

Clinical studies of beta-thioguanine deoxyriboside alone and in combination with arabinosyl cytosine.

Medical and pediatric oncology, 1976, Volume: 2, Issue:2

Beta-thioguanine deoxyriboside (betaTGdR) is a purine nucleoside derivative which was studied alone or in combination with arabinosyl cytosine (Ara-C) in patients with solid tumors and acute leukemia. No significant responses were observed in 22 patients with solid tumors. The response rate with betaTGdR alone in acute leukemia was 26% and in combination with Ara-C was 24%. Responses were generally of short duration. Toxicity included myelosuppression, nausea, stomatitis, hyperpigmentation, photosensitivity, and liver function abnormalities.

Topics: Acute Disease; Adolescent; Adult; Aged; Child; Child, Preschool; Cytarabine; Deoxyguanosine; Deoxyribonucleosides; Drug Therapy, Combination; Female; Guanosine; Humans; Leukemia; Leukopenia; Male; Middle Aged; Neoplasm Metastasis; Neoplasms; Remission, Spontaneous; Thioguanine; Thionucleosides; Thrombocytopenia; Time Factors

1976