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Abemaciclib, an inhibitor of cyclin dependent kinases 4 and 6, is indicated for metastatic breast cancer treatment. Reversible increases in serum creatinine levels of approximately 15%-40% over baseline have been observed following abemaciclib dosing. This study assessed the in vitro and clinical inhibition of renal transporters by abemaciclib and its metabolites using metformin (a clinically relevant transporter substrate), in a clinical study that quantified glomerular filtration and iohexol clearance, In vitro, abemaciclib inhibited metformin uptake by OCT2, MATE1 and MATE2-K transporters with an IC50 of 0.4-3.8 μM. Clinically abemaciclib significantly increased metformin exposure but did not significantly affect measured glomerular filtration rate, serum NGAL, serum cystatin C or the urinary markers of kidney tubular injury, NGAL and KIM-1,. This article is protected by copyright. All rights reserved.
This article was published in the following journal.
Name: Clinical pharmacology and therapeutics
Following reversal of short periods of ureteral obstruction (UO), glomerular and tubular renal dysfunction recovers with time. Diabetes mellitus (DM) affects glomerular functions; thus, it is possible...
One of the first structural changes in diabetic nephropathy (DN) is the renal enlargement. These changes resulted in renal hypertrophy in both glomerular and tubular cells. Shrink in the kidney size, ...
The qualitative evaluation of proteinuria represents a crucial diagnostic step in clinical practice for the classification of renal diseases according to glomerular, tubulo-interstitial, mixed injury ...
To maintain electrolyte homeostasis, the kidneys reabsorb more than 99% of the filtered Na under physiological conditions, resulting in less than 1% of the filtered Na excreted in urine. In contrast, ...
Lonomia obliqua venom is nephrotoxic and acute kidney injury (AKI) is the main cause of death among envenomed victims. Mechanism underlying L. obliqua-induced AKI involves renal hypoperfusion, inflamm...
Cisplatin is a heavy-metal complex widely used in the treatment of a variety of malignancies, including small cell and non-small cell lung cancer, ovarian, bladder, head and neck, esophage...
The investigators aim at describing changes in renal glomerular and tubular function with after the switch from TDF to TAF in HIV/HBV-coinfected patients with mild to moderate renal dysfun...
Acute Renal Failure (ARF) is defined by a severe, and usually reversible, glomerular filtration rate decreasing. Acute Tubular Necrosis (ATN) remain the major cause of ARF involving distre...
High dose methotrexate (MTX) is responsible of severe toxicity in patients in whom elimination from plasma is delayed. Factors responsible for MTX accumulation are partly known but some pa...
Aim of the present study is to determine whether 1. RRI can predict glomerular hyperfiltration; 2. glomerular hyperfiltration is associated with low renal resistive index; 3...
The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.
A cytosolic carbonic anhydrase isoenzyme found widely distributed in cells of almost all tissues. Deficiencies of carbonic anhydrase II produce a syndrome characterized by OSTEOPETROSIS, renal tubular acidosis (ACIDOSIS, RENAL TUBULAR) and cerebral calcification. EC 4.2.1.-
Conditions in which the KIDNEYS perform below the normal level in the ability to remove wastes, concentrate URINE, and maintain ELECTROLYTE BALANCE; BLOOD PRESSURE; and CALCIUM metabolism. Renal insufficiency can be classified by the degree of kidney damage (as measured by the level of PROTEINURIA) and reduction in GLOMERULAR FILTRATION RATE. The most severe form is KIDNEY FAILURE. Renal function may deteriorate slowly (RENAL INSUFFICIENCY, CHRONIC) or precipitously (RENAL INSUFFICIENCY, ACUTE).
A condition characterized by calcification of the renal tissue itself. It is usually seen in distal RENAL TUBULAR ACIDOSIS with calcium deposition in the DISTAL KIDNEY TUBULES and the surrounding interstitium. Nephrocalcinosis causes RENAL INSUFFICIENCY.
Inflammation of the interstitial tissue of the kidney. This term is generally used for primary inflammation of KIDNEY TUBULES and/or surrounding interstitium. For primary inflammation of glomerular interstitium, see GLOMERULONEPHRITIS. Infiltration of the inflammatory cells into the interstitial compartment results in EDEMA, increased spaces between the tubules, and tubular renal dysfunction.
Chronic kidney disease (CKD), also known as chronic renal disease, is a progressive loss in renal function over a period of months or years. The symptoms of worsening kidney function are non-specific, and might include feeling generally unwell and experi...