Canagliflozin is a medication used to treat type 2 diabetes. It is a third-line medication to be tried after metformin, a first-line medication for type 2 diabetes. It is used together with exercise and diet. It is not recommended in type 1 diabetes.

Mechanism action of Canagliflozin

Canagliflozin is a sodium-glucose cotransporter (SGLT2) inhibitor. Glucose filtered in the renal tubular lumen is mainly reabsorbed by SGLT2 expressed in the proximal renal tubule. By inhibiting SGLT2, cagliegin reduces the renal reabsorption of filtered glucose, lowers renal glucose threshold (RTG) and increases urine glucose excretion, thus reducing blood glucose.

It is important to note that SGLT2 inhibitors are safe because their hypoglycemic effect is insulin-independent and fasting increases compensatory production of hepatic endogenous glucose.

What are the effects of Canagliflozin?

Lower blood sugar

As a new type of hypoglycemic drug, Canagliflozin has obvious advantages compared with other drugs. Traditional hypoglycemic drugs keep sugar in the human body, while this type of drug directly excretes sugar through the kidneys, and only when the blood sugar exceeds the kidneys. When the glucose threshold is reached, the hypoglycemic effect is exerted, and the hypoglycemic effect is not stimulated by insulin secretion, so it will not cause the risk of hypoglycemia, so as to achieve the good effect of fast and safe hypoglycemia.

Cardiovascular protection

Several studies have shown that SGLT2 inhibitors have cardioprotective effects and can be used in the treatment of heart failure, not only improving patient outcomes, but also reducing hospitalization and mortality, and for heart failure with or without diabetes. certain effect. In addition, it also has the effect of improving atherosclerosis, myocardial energy metabolism and anti-fibrosis.

 Antihypertensive effect

Clinical data show that Canagliflozin can reduce systolic blood pressure to varying degrees, and the reduction is significantly dose-dependent. For example, in the clinical trial of canagliflozin, compared with the placebo group, the reduction in systolic blood pressure was between 2.6-5.7 mmHg at a dose of 100 mg, and at a dose of 300 mg, the reduction in systolic blood pressure reached 3.5-7.9 between mmHg.

On the one hand, its mechanism of action is to lower blood pressure through urinary sodium excretion, and on the other hand, it has a hypotensive effect by reducing inflammation and oxidative stress, improving vascular cell function and reducing arteriosclerosis. While exerting antihypertensive effect, it will not cause hyponatremia.

Weight loss

Canagliflozin reduce energy through the action of urine sugar, and at the same time induce the browning of white adipose tissue. Since there are two main types of fat in humans, namely white fat and brown fat, the former stores energy and the latter produces heat and consumes energy, so brown fat is increased. Quantity can increase energy consumption, improve metabolism, and achieve weight loss.

Decreased uric acid

Canagliflozin can lead to increased uric acid excretion, reducing uric acid in the body. However, compared with the classic uric acid-lowering drugs, its effect is relatively weak, so it is more promising to be used in patients with asymptomatic hyperuricemia or diabetes complicated with hyperuricemia.

Liver protection

SGLT2 inhibitors can protect the liver by altering the glucose-fatty acid cycle, increasing the utilization and oxidation of fatty acids in skeletal muscle, adipose tissue and the liver, thereby reducing the accumulation of fatty acids in the liver. Clinical data show that SGLT2 inhibitors can prevent and treat nonalcoholic fatty liver disease to a certain extent.

Huateng Pharma is a leading and professional manufacturer which can provide pharmaceutical intermediates, PEG derivatives, biochemical reagents, APIs, Vitamin D Derivatives and so on. After research and development, Huateng Pharma can provide the following four intermediates of Canagliflozin at present.

(5-Bromo-2-methylphenyl)[5-(4-fluorophenyl)-2-thienyl]methanone

CAS NO.1132832-75-7

2-(4-Fluorophenyl)-5-[(5-iodo-2-methylphenyl)methyl]thiophene

CAS NO.898566-17-1

2-[(5-bromo-2-methylphenyl)methyl]-5-(4-fluorophenyl)thiophene

CAS NO.1030825-20-7

2-(4-Fluorophenyl)thiophene

CAS NO.58861-48-6