Direct labeling of isoniazid with technetium-99m for diagnosis of tuberculosis

Roohi, Samina; Ahmad, Masood; Jehangir, M.; Malik, Salman Akbar

doi:10.1524/ract.2006.94.3.147

Cited by 16 publications

(9 citation statements)

References 12 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Other studies in mice with i.v. administration show drug concentrations in the liver, lung and kidney that are several fold higher than the amounts estimated using PET imaging,34 while Roohi et al used a technetium-99m derivative of INH to determine the drug biodistribution in Sprague-Dawley rats giving similar drug concentrations in heart and lung but more than 10-fold higher concentrations in the liver and kidney compared to the other studies 35. Again, interspecies variation could play an important role in any differences observed between our study and those conducted in rodents, with the additional caveat that the study in rats involved the use of INH that had been modified with technetium-99m.…”

Section: Resultsmentioning

confidence: 99%

Radiosynthesis and Bioimaging of the Tuberculosis Chemotherapeutics Isoniazid, Rifampicin and Pyrazinamide in Baboons

Liu

Xu²,

Shea³

et al. 2010

J. Med. Chem.

View full text Add to dashboard Cite

The front-line tuberculosis (TB) chemotherapeutics isoniazid (INH), rifampicin (RIF) and pyrazinamide (PZA) have been labeled with carbon-11 and the biodistribution of each labeled drug has been determined in baboons using positron emission tomography (PET). Each radiosynthesis and formulation has been accomplished in 1 h, using [11C]CH3I to label RIF, and [11C]HCN to label INH and PZA. Following i.v. administration, INH, PZA, RIF and/or their radiolabeled metabolites clear rapidly from many tissues, however INH, PZA and/or their metabolites accumulate in the bladder while RIF and/or its metabolites accumulates in the liver and gall bladder, consistent with the routes of excretion of the drugs. In addition, the biodistribution data demonstrate that the ability of the three drugs and their radiolabeled metabolites to cross the blood-brain barrier decreases in the order PZA > INH > RIF, although in all cases the estimated drug concentrations are greater than the minimum inhibitory concentration (MIC) values for inhibiting bacterial growth. The pharmacokinetic (PK) and drug distribution data have important implications for treatment of disseminated TB in the brain, and pave the way for imaging the distribution of the pathogen in vivo.

show abstract

Section: Resultsmentioning

confidence: 99%

Radiosynthesis and Bioimaging of the Tuberculosis Chemotherapeutics Isoniazid, Rifampicin and Pyrazinamide in Baboons

Liu

Xu²,

Shea³

et al. 2010

J. Med. Chem.

View full text Add to dashboard Cite

show abstract

“…It was chosen as ligand for 99m Tc-labeling and imaging in the developed animal model with a gamma camera. The results suggested that 99m Tc-isoniazid was a specific agent for localization of tubercular lesions [66]. Kanamycin is an antibiotic used for treatment of infections when penicillin or other less toxic drugs cannot be used.…”

Section: Labelling Procedures and Kit Formulationsmentioning

confidence: 97%

Development of radiochemistry in Pakistan – 1960 to 2010

et al. 2012

Self Cite

View full text Add to dashboard Cite

Development of radiochemistry / Uranium and thorium chemistry / Nuclear reaction cross section / Radioisotope and radiopharmaceutical production / Neutron activation analysis / Separation studies / PINSTECHSummary. With the inception of Pakistan Atomic Energy Commission (PAEC) in 1956, peaceful uses of atomic energy commenced for the benefit of scientific community as well as masses of Pakistan. Radiochemistry played a vital role right from the beginning. The research and development in this field accelerated soon after the criticality of the first research reactor named as Pakistan Research Reactor (PARR-1) at the Pakistan Institute of Nuclear Science and Technology (PINSTECH), Islamabad. The first radioisotope produced at PARR-1 for application in nuclear medicine was 131 I. Later on, many other radioisotopes were prepared and radiopharmaceuticals were synthesised for their use in industry and hospitals. Besides providing pure radioactive tracers for nuclear medicine, radiochemistry also enhanced the detection limit of impurities at all stages of nuclear fuel cycle for power generation. In 1983, research in the field of nuclear data measurement began. The main aim was to identify suitable conditions for the production of radionuclides for cancer diagnostics, treatment and therapy. With the establishment of a second research reactor (PARR-2) at PINSTECH, research in neutron activation analysis, radioisotope production and separation studies gained more momentum and many research articles were published. Solvent extraction, adsorption and ion-exchange were the main routes of separation in those studies. Separation of heavy metals and treatment of waste generated in a nuclear power plant are other important aspects related to environmental restoration and nuclear waste management, where radiochemistry is required. In future, work in radiochemistry will be continued on similar lines to develop novel radiopharmaceuticals, identify indigenous schemes for nuclear waste management and work out intelligent procedures for material characterization for benefit to mankind, especially the people of Pakistan.

show abstract

“…177 Lu emits both beta (β) and gamma (γ) particles; β‐particle emissions ( E max = 487, 383 and 175 keV) are used for remedy purpose of tumor and bone ache palliation, etc. and γ‐radiation (113 and 208 keV) for imaging …”

Section: Introductionmentioning

confidence: 99%

Radiolabeling, quality control, and biological characterization of ¹⁷⁷Lu‐labeled kanamycin

et al. 2017

Self Cite

View full text Add to dashboard Cite

Kanamycin is an antibiotic, isolated from Streptomyces kanamyceticus, which is used to treat serious bacterial infections. The fact that the present radioligand Tc-kanamycin used for diagnosis is short-lived, raised a need to label and study kanamycin with one of the most important beta (β) radiation emitting isotope Lu. Labeling yield of Lu-kanamycin was confirmed by different chromatography techniques such as paper chromatography, TLC, HPLC. Several experiments were performed to optimize labeling with changing reaction conditions such as pH, temperature, amount of ligand, and reaction time. In vitro stability analysis was performed incubation with human serum. Electrophoresis analysis was also conducted to determine the charge on Lu-kanamycin. The biodistribution and scintigraphy were performed in normal mice and rabbit, respectively, at different time intervals of postinjection. Lu-kanamycin was prepared with very high yield (~100%), with excellent stability in vivo and in vitro (>99% 6 hr postprep.), at pH 7. Maximum labeling was achieved at less reaction time (15 min), with maximum conjugation of the ligand (12.5 mg) with Lu. Electrophoresis analysis showed net neutral charge. The radioligand showed rapid clearance from body in biodistribution and scintigraphy studies. The preparation Lu-kanamycin could be used as a radio-pharmaceutical for infection imaging purpose, especially when transporting the radioligand to long-range distances.

show abstract

Direct labeling of isoniazid with technetium-99m for diagnosis of tuberculosis

Abstract: SummaryIsonicotinic acid hydrazide (isoniazid) is one of the most effective agents in tuberculosis therapy. Hence it was chosen as ligand for

Cited by 16 publications

References 12 publications

Radiosynthesis and Bioimaging of the Tuberculosis Chemotherapeutics Isoniazid, Rifampicin and Pyrazinamide in Baboons

Radiosynthesis and Bioimaging of the Tuberculosis Chemotherapeutics Isoniazid, Rifampicin and Pyrazinamide in Baboons

Development of radiochemistry in Pakistan – 1960 to 2010

Radiolabeling, quality control, and biological characterization of ¹⁷⁷Lu‐labeled kanamycin

Contact Info

Product

Resources

About

Direct labeling of isoniazid with technetium-99m for diagnosis of tuberculosis

Abstract: SummaryIsonicotinic acid hydrazide (isoniazid) is one of the most effective agents in tuberculosis therapy. Hence it was chosen as ligand for

Cited by 16 publications

References 12 publications

Radiosynthesis and Bioimaging of the Tuberculosis Chemotherapeutics Isoniazid, Rifampicin and Pyrazinamide in Baboons

Radiosynthesis and Bioimaging of the Tuberculosis Chemotherapeutics Isoniazid, Rifampicin and Pyrazinamide in Baboons

Development of radiochemistry in Pakistan – 1960 to 2010

Radiolabeling, quality control, and biological characterization of 177Lu‐labeled kanamycin

Contact Info

Product

Resources

About

Radiolabeling, quality control, and biological characterization of ¹⁷⁷Lu‐labeled kanamycin