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Carboplatin dosage: prospective evaluation of a simple formula based on renal function.
TLDR
The formula provides a simple and consistent method of determining carboplatin dose in adults and will not be influenced by previous or concurrent myelosuppressive therapy or supportive measures, and is applicable to combination and high-dose studies as well as conventional single-agent therapy, although the target AUC will need to be redefined for combination chemotherapy.
Preclinical evaluation of a potent novel DNA-dependent protein kinase inhibitor NU7441.
TLDR
NU7441 shows sufficient proof of principle through in vitro and in vivo chemos Sensitization and radiosensitization to justify further development of DNA-PK inhibitors for clinical use.
Anticancer chemosensitization and radiosensitization by the novel poly(ADP-ribose) polymerase-1 inhibitor AG14361.
TLDR
AG14361 is, to the authors' knowledge, the first high-potency PARP-1 inhibitor with the specificity and in vivo activity to enhance chemotherapy and radiation therapy of human cancer.
Phase I Study of the Poly(ADP-Ribose) Polymerase Inhibitor, AG014699, in Combination with Temozolomide in Patients with Advanced Solid Tumors
TLDR
The combination of AG014699 and temozolomide is well tolerated, pharmacodynamic assessments showing proof of principle of the mode of action of this new class of agents is shown.
COMPROMISED CDK1 ACTIVITY SENSITIZES BRCA-PROFICIENT CANCERS TO PARP INHIBITION
TLDR
Combined inhibition of Cdk1 and PARP in BRCA–wild-type cancer cells resulted in reduced colony formation, delayed growth of human tumor xenografts and tumor regression with prolonged survival in a mouse model of lung adenocarcinoma.
Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles.
TLDR
CDK inhibition and chemosensitivity data indicate that the distinct mode of binding of NU2058 and NU6027 has direct consequences for enzyme and cell growth inhibition.
Pharmacokinetics of cis-diammine-1,1-cyclobutane dicarboxylate platinum(II) in patients with normal and impaired renal function.
TLDR
In vitro studies with plasma and urine demonstrated that, in contrast to cisplatin, CBDCA is a stable complex [t 1/2 - 37 degrees; plasma, 30 hr, and urine, 20 to 460 hr].
Temozolomide Pharmacodynamics in Patients with Metastatic Melanoma: DNA Damage and Activity of Repair Enzymes O6-Alkylguanine Alkyltransferase and Poly(ADP-Ribose) Polymerase-1
TLDR
ParP activity was not inhibited by temozolomide treatment and this newly validated pharmacodynamic assay is therefore suitable for use in a proof-of-principle phase I trial a PARP-1 inhibitor in combination with temozOLomide.
Propylene Glycol Pharmacokinetics and Effects after Intravenous Infusion in Humans
TLDR
A rapid gas chromatographic assay method is described for PG and the plasma pharmacokinetics after intravenous administration to six patients on nine occasions, finding no evidence of lactic acidosis, hemolysis, or increase in osmolality at 3–15 g/m2 PG infused over periods of 4 h.
Preclinical selection of a novel poly(ADP-ribose) polymerase inhibitor for clinical trial
TLDR
A compound, AG14447, is identified as a PARP inhibitor with outstanding in vivo chemosensitization potency at tolerable doses, which is at least 10 times more potent than the initial lead,AG14361.
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