U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Ixazomib (trade name Ninlaro) is a drug for the treatment of multiple myeloma in adults after at least one prior therapy, in combination with lenalidomide and dexamethasone. It is taken by mouth in form of capsules. Common side effects include diarrhea, constipation and low platelet count. Like the older bortezomib (which can only be given by injection), it acts as a proteasome inhibitor, has orphan drug status in the US and Europe. At therapeutic concentrations, ixazomib selectively and reversibly inhibits the protein proteasome subunit beta type-5 (PSMB5) with a dissociation half-life of 18 minutes. This mechanism is the same as of bortezomib, which has a much longer dissociation half-life of 110 minutes; the related drug carfilzomib, by contrast, blocks PSMB5 irreversibly. Proteasome subunits beta type-1 and type-2 are only inhibited at high concentrations reached in cell culture models. PSMB5 is part of the 20S proteasome complex and has enzymatic activity similar to chymotrypsin. It induces apoptosis, a type of programmed cell death, in various cancer cell lines. A synergistic effect of ixazomib and lenalidomide has been found in a large number of myeloma cell lines. The medication is taken orally as a prodrug, ixazomib citrate, which is a boronic ester; this ester rapidly hydrolyzes under physiological conditions to its biologically active form, ixazomib, a boronic acid. Absolute bioavailability is 58%, and highest blood plasma concentrations of ixazomib are reached after one hour. Plasma protein binding is 99%.
Status:
US Approved OTC
Source:
21 CFR 331.11(e) antacid:citrate-containing citrate (containing active ingredients: citrate ion, as citric acid or salt)
Source URL:
First marketed in 1921
Source:
Potassium Citrate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Potassium citrate is indicated for the management of renal tubular acidosis with calcium stones, hypocitraturic calcium oxalate nephrolithiasis of any etiology, uric acid lithiasis with or without calcium stones. WhenPotassium citrate is given orally, the metabolism of absorbed citrate produces an alkaline load. The induced alkaline load in turn increases urinary pH and raises urinary citrate by augmenting citrate clearance without measurably altering ultrafilterable serum citrate. Thus, potassium citrate therapy appears to increase urinary citrate principally by modifying the renal handling of citrate, rather than by increasing the filtered load of citrate. Potassium citrate is used as a food additive (E 332) to regulate acidity.
Struvite, a crystalline substance first identified in the 18th century, is composed of magnesium ammonium phosphate. Struvite urinary stones are also known as ‘infection stones’, and account for 15%-20% of all urinary stones. Bacterial urease, usually from a Proteus species, is responsible for the chemical changes in urine which result in struvite formation.
Status:
US Approved OTC
Source:
21 CFR 331.11(e) antacid:citrate-containing citrate (containing active ingredients: citrate ion, as citric acid or salt)
Source URL:
First marketed in 1921
Source:
Potassium Citrate U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Potassium citrate is indicated for the management of renal tubular acidosis with calcium stones, hypocitraturic calcium oxalate nephrolithiasis of any etiology, uric acid lithiasis with or without calcium stones. WhenPotassium citrate is given orally, the metabolism of absorbed citrate produces an alkaline load. The induced alkaline load in turn increases urinary pH and raises urinary citrate by augmenting citrate clearance without measurably altering ultrafilterable serum citrate. Thus, potassium citrate therapy appears to increase urinary citrate principally by modifying the renal handling of citrate, rather than by increasing the filtered load of citrate. Potassium citrate is used as a food additive (E 332) to regulate acidity.
Status:
US Approved OTC
Source:
21 CFR 331.11(c)(3) antacid:bismuth-containing bismuth subcarbonate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Bibrocathol (trade names Noviform and Posiformin) is a well-established topical antiseptic for the treatment of acute eyelid diseases like blepharitis. Eye ointments containing 2 or 5 % bibrocathol and the excipients liquid paraffin, white soft paraffin, and lanolin have been marketed since 1967 for the treatment of eye irritation, chronic blepharitis, and uninfected corneal injuries. Reports of clinical experience with bibrocathol for inflammation of the edge of the palpebra exist since the beginning of the 20th century. Until recently, no controlled, randomized clinical studies according to the guidelines for Good Clinical Practice for Trials on Medical Products for Human Use (GCP) as defined by the International Conference on Harmonisation (ICH) have been performed with bibrocathol 2 % ointment, as these were not required for marketing authorization in the 1960s. A first double-blind, prospective, controlled, GCP-compliant clinical study was recently performed to assess the efficacy of bibrocathol 5 % (Noviform®) in acute blepharitis. It demonstrated superior efficacy of bibrocathol 5 % ointment as compared to an ointment vehicle (placebo) after 2 weeks of treatment as assessed by a combined measure of slit-lamp examination results and patients’ subjective complaints.
mixture
Status:
US Approved OTC
Source:
21 CFR 331.11(e) antacid:citrate-containing citrate (containing active ingredients: citrate ion, as citric acid or salt)
Source URL:
First marketed in 1921
Source:
Potassium Citrate U.S.P.
Source URL:

Class:
MIXTURE



Potassium citrate is indicated for the management of renal tubular acidosis with calcium stones, hypocitraturic calcium oxalate nephrolithiasis of any etiology, uric acid lithiasis with or without calcium stones. WhenPotassium citrate is given orally, the metabolism of absorbed citrate produces an alkaline load. The induced alkaline load in turn increases urinary pH and raises urinary citrate by augmenting citrate clearance without measurably altering ultrafilterable serum citrate. Thus, potassium citrate therapy appears to increase urinary citrate principally by modifying the renal handling of citrate, rather than by increasing the filtered load of citrate. Potassium citrate is used as a food additive (E 332) to regulate acidity.