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Lipaglyn (Saroglitazar) for Treating Hypertriglycerdemia in Type II Diabetes

Lipaglyn™ (Saroglitazar) is a dual peroxisome proliferator-activated receptor (PPAR) agonist indicated for the treatment of hypertriglyceridemia in Type II diabetics.

Drug Name (Brand / Generic)

Lipaglyn / saroglitazar

Developed By

Zydus Cadila

Therapy Class

Dual PPAR agonist

Current Indication

Diabetic dyslipidemia or hypertriglyceridemia in type II diabetes

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Lipaglyn™ (Saroglitazar) is a dual peroxisome proliferator-activated receptor (PPAR) agonist indicated for the treatment of hypertriglyceridemia in Type II diabetics.

The drug was discovered and developed by Zydus Cadila, a pharmaceutical company in India.

Zydus Cadila submitted a new drug application (NDA) for Lipaglyn’s approval to the Drug Controller General of India (DCGI) in 2012. It received marketing approval for Lipaglyn from the DCGI for treating diabetic dyslipidemia in Type II diabetics in June 2013.

Zydus received marketing approval for Lipaglyn™ in Mexico in November 2017 to treat dyslipidemia in type 2 diabetics and hypertriglyceridemia in type 2 diabetics uncontrolled by statins.

Zydus is also evaluating the use of Lipaglyn™ to treat liver conditions such as non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD) and primary biliary cholangitis (PBC). In December 2019, the company submitted an application to the DCGI seeking approval for Saroglitazar Magnesium (Mg) to treat NASH.

“Lipaglyn was discovered and developed by Zydus Cadila, a pharmaceutical company in India.

Hypertriglyceridemia in type II diabetics

Hypertriglyceridemia, also known as diabetic dyslipidemia, is a condition whereby a person with diabetes has high blood lipid levels or triglycerides.

The elevated level of triglycerides is one of the major risk factors associated with cardiovascular diseases (CVD).

India is estimated to have approximately 65 million people with diabetes, with more than 80% of them suffering from diabetic dyslipidemia. An estimated 85% of diabetics in the world suffer from diabetic dyslipidemia.

It was also found that about 30% of deaths in the world are caused by CVD and diabetes is one of the major causes associated with CVD.

Lipaglyn’s (saroglitazar) mechanism of action

Lipaglyn™ contains two main classes of PPAR agonists, which include PPARα (alpha) and PPARγ (gamma). The drug has both lipid and glucose-lowering effects in a single molecule. It lowers the high blood triglycerides as well as blood sugar and improves the insulin resistance. The drug is available in tablet form of 4mg dose for oral administration.

In NASH models, the drug was observed to act on all disease components such as steatosis, ballooning, inflammation and fibrosis.

“Lipaglyn™ contains two main classes of PPAR agonists, which include PPARα (alpha) and PPARγ (gamma).

Clinical trials on Zydus’s Lipaglyn (saroglitazar)

The approval for Lipaglyn™ in diabetic dyslipidemia indication was based on the results obtained from clinical studies, which were conducted for more than eight years. The studies evaluated the efficacy, safety, pharmacokinetics and pharmacodynamics of the drug.

Phase I clinical trials on Lipaglyn™ were conducted in 2005 and Phase II studies were completed in 2006. The Phase III clinical trials were conducted between 2008 and 2011.

The first Phase III clinical trials on Lipaglyn™ compared Lipaglyn™ 4mg dose with pioglitazone, a similar drug developed by Takeda.

The results of the study demonstrated that patients who were administered with Lipaglyn™ 4mg dose showed a reduction in LDL cholesterol and triglycerides and an increase in HDL cholesterol. The study also showed that Lipaglyn-administered patients showed a reduction in fasting plasma glucose and glycosylated haemoglobin.

The second Phase III clinical trials on Lipaglyn™ were conducted to evaluate the diabetic dyslipidemic patients insufficiently controlled with statin therapy.

The second Phase III study results showed that patients treated with Lipaglyn™ showed a pronounced beneficial effect on both the lipid and glycaemic parameters.

Lipaglyn was well tolerated and the safety profile of the drug was shown to be better than its comparator drugs in both trials. It was also found that the drug had a non-renal route of elimination and didn’t show adverse events such as oedema, weight gain, myopathies, or derangement of liver or kidney functions, thus making it safe and efficacious.

In Phase II trials involving NAFLD patients, Saroglitazar Mg improved liver enzymes and also demonstrated favorable effects on lipid and glycemic indices.

The drug also yielded positive data in Phase III biopsy-driven EVIDENCES II study, which compared 4 mg Saroglitazar to placebo in participants suffering from NASH.

Furthermore, Zydus is conducting a Phase II study, named EVIDENCES VII, of Saroglitazar magnesium (Saroglitazar Mg) to treat NAFLD in women with polycystic ovary syndrome (PCOS).

Marketing commentary for India’s Zydus Cadila

Zydus Cadila, part of Zydus Group, is a leading international pharmaceutical company with its headquarters located in Ahmadabad, India. The company discovers, develops, produces and markets a wide range of healthcare therapies.

Zydus Cadila launched Lipaglyn across the Indian market in 2013. The company spent about $250m for the development of Lipaglyn™.

It committed to spend between another $150m and $200m to launch the drug in overseas markets.

Lipaglyn™ is expected to be a blockbuster drug in the coming years. The drug is expected to have $30bn market globally. The drug will face competition from Takeda’s Actos (pioglitazone).

 


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