Generated: May 24, 2017
|Title:||Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy|
|Abstract:||The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N--CH2COCH2-CH2CO--OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.|
|Inventor(s):||Gierskcky; Karl E. (Hosle, NO), Moan; Johan (Oslo, NO), Peng; Qian (Oslo, NO), Steen; Harald (Oslo, NO), Warloe; Trond (Oslo, NO), Bjorseth; Alf (Oslo, NO)|
|Assignee:||PhotoCure ASA (Oslo, NO)|
1. A method of diagnosing urinary bladder abnormalities in a patient in need thereof comprising: a. collecting cells from urine of the patient by centrifugation; b. mixing the cells
with a solution comprising 0.04 mg hexyl aminolevulinate hydrochloride per ml of cell growth medium containing 10% fetal calf serum, pH 7.2; c. incubating the mixture for about 4 hours; d. shining light with a wavelength of 390-440 nm on the incubated
mixture; e. determining whether any of the cells fluoresce in the wavelength range 620-640 nm.
2. The method of claim 1 wherein the abnormality is carcinoma in situ.
3. A method of diagnosing urinary bladder abnormalities in a patient in need thereof comprising: a. instilling into the patient's bladder a solution comprising 4.3 mM KH.sub.2PO.sub.4, 4.3 mM Na.sub.2HPO.sub.4, 120 mM NaCl, pH 6.0, and 8 mM hexyl aminolevulinate; b. leaving the solution in the bladder for one hour; c. evacuating the bladder; d. identifying potential lesions by inspecting and mapping all areas that fluoresce under light of wavelength in the range 380 to 450 nm; and e. optionally confirming the presence of lesions by having biopsies performed on the suspected lesions.
4. The method of claim 3 wherein the abnormality is carcinoma in situ.
5. A method of treating urinary bladder abnormalities responsive to photochemotherapy in a patient in need thereof comprising: a. introducing into a patient's bladder a solution comprising 0.1 to 1.0 mmol of hexyl aminolevulinate hydrochloride in 50 ml phosphate buffered saline, pH 6.0; b. allowing the solution to remain in the urinary bladder for a period of 5 minutes to 4 hours; c. removing the solution from the bladder; d. inspecting the bladder with white light and with blue light having wavelength between 375 and 440 nm; e. resecting the papillary and superficial lesions optionally performing the resection under blue light; f. where the resection is not performed under blue light, checking the resected lesions by HAL imaging; g. exposing the lesions to white light, red light of wavelength 630-635 nm, or blue light of wavelength 375-440 nm, to provide a total light dose of 10-100 J/cm.sup.2 with a fluence of 50-200 mW/cm.sup.2, wherein the light is applied either locally to each lesion or to the entire bladder.
6. The method of claim 5 wherein the abnormality is carcinoma in situ.
7. The method of claim 5 wherein the abnormality is a bacterial, viral, or fungal infection, or an abnormality characterized by discrete lesions.
8. The method of claim 5 wherein the abnormality is bladder cancer.
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