An analysis of lecture topics over five decades of the European Federation for Medicinal Chemistry International Symposium on Medicinal Chemistry reveals shifts in the importance given to therapeutic areas, treatment modalities, and technologies.

A historical overview of key events that led, 50 years ago, to the foundation of the European Federation for Medicinal Chemistry (EFMC), and the impact this had on promoting and structuring medicinal chemistry as a discipline in Europe.

For all those who are interested in the recent history of the pharmaceutical and biotechnology industry in India, and who want to go beyond annual reports and corporate presentations, four recently published biographies are must-reads. Whereas three books are autobiographies, a fourth one is the result of countless interviews of key players (scientists, current and past coworkers, pharma rivals, ministries, etc…), and gives unique insights into the development of biotechnology in India.

A comprehensive survey of proprietary drug discovery and development efforts by Indian companies between 1994 and mid-2016, focusing on preclinical and clinical development compounds by company, therapeutic indication, mode of action, target class, and development status. The analysis includes the evolution of the overall pipeline over two decades, attrition rates, in-house developments and contributions to Western pharmaceutical pipelines through licensing agreements.

Global pharmaceutical companies including Hoffmann-La Roche, Boehringer Ingelheim, or Pierre Fabre have recently signed major licensing deals with Indian biotech companies to acquire the rights to preclinical development candidates. Cancer is the leading therapeutic indication covered by these deals, with approaches ranging from immuno-oncology to epigenetics, and covering both small molecules and peptides.

Aurigene Discovery Technologies, the Bangalore-based biotech company, and Pierre Fabre, the second largest independent French pharmaceutical company, announced on February 11, 2014, a collaborative license, development and commercialization agreement giving Pierre Fabre worldwide rights (excluding India) to a new immune checkpoint modulator, AUNP-12, for the treatment of cancer. Aurigene will receive an upfront payment as well as milestone payments based upon continued development, regulatory progress, and product commercialization.

Global pharmaceutical and biotechnology companies have been building increasingly on the skills and services offered by Indian biotech companies through strategic collaborative partnerships and alliances to fuel their in-house discovery and development pipelines. With the exception of generic press releases, however, very little has been published on the process and progress of drug discovery itself, such as the targets or modes of action involved, nor on the scientific output of such collaborations, and therefore on new chemical entities coming out of India through research collaborations. In this review, we have analyzed recent patents, patent applications, and peer-reviewed publications of major research alliances, with the aim of highlighting their scientific output as well as the considerable bandwidth of targets and therapeutic areas involved.

In this Conference Report on ASMC'13 Moscow (May 5–8, 2013), we aim at highlighting new synthetic methodologies and at expanding the drug discovery space from small to large molecules, including carbohydrates, novel protein scaffolds, dendrimers, and genes.

According to the eleventh annual Indian Biotech Industry survey by Biospectrum-ABLE (Association of Biotechnology Led Enterprises), the Indian biotech industry grew by 15.1 % in 2012-13, increasing its revenues from 204.4 Billion INR (Indian Rupees) to 235.24 Billion INR (3.94 B US$).

Zydus Cadila announced on June 5 2013 the approval by the Drug Controller General of India (DCGI) of Saroglitazar (ZYH1), or Lipaglyn^TM. The drug has been approved for launch in India for the treatment of diabetic dyslipidemia or hypertriglyceridemia in patients with type II diabetes not controlled by statins alone [1] .

Lipaglyn^TM is the first glitazar to be approved in the world, and is the first NCE discovered and developed indigenously by an Indian company. The drug originates from a research program initiated at Zydus Cadila in 2000, and an IND submission in 2004 after extensive structure-activity relationship studies and preclinical characterization.

The compound belongs to the class of ‘glitazars’, dual peroxisome proliferator-activated receptor (PPAR) agonists with affinity towards both PPARα and PPARγ [2] [3]. According to Zydus Cadila [1], Saroglitazar has a predominant affinity for the PPARα isoform, and a moderate affinity for PPARγ, and has shown beneficial effects on lipids and glycemic controls without side effects. At a dose of 4 mg once daily, it reduces triglycerides and LDL cholesterol, it increases HDL cholesterol, and also shows a reduction in Fasting Plasma Glucose and glycosylated hemoglobin.

Ranbaxy has recently launched India’s first domestically developed drug, Synriam, a fixed dose combination of arterolane maleate and piperaquine phosphate. The drug has been approved in 2011 by the Drug Controller General of India for treating Plasmodium falciparum malaria. Although developed in India, Arterolane itself was not discovered in India, but by a collaborative drug discovery project funded by the Medicines for Malaria Venture (MMV), a Swiss charity, which in 2003 partnered with Ranbaxy to carry out the development, before backing out of developing the drug further in 2007, granting a world-wide license to Ranbaxy.

Glenmark and US partner Salix Pharmaceuticals gained approval by FDA in December 2012 of Crofelemer, for the treatment of non-infectious diarrhea in patients taking antiretroviral therapy for HIV/AIDS. Crofelemer, a purified oligomeric proanthocyanidin (MW up to 9 kDa), isolated from the latex of the South American Croton lechleri tree, has a new mechanism of action, blocking two structurally unrelated chloride channels in the gut, thereby decreasing the excretion of water, and reducing the duration of the diarrhea.

These are only the two first visible signs of India’s growing presence in innovative drug discovery and development, which started in the late nineties, and became rapidly known in the early 2000’s with some high profile licensing deals with Western pharmaceutical companies.

According to the tenth annual Indian Biotech Industry survey by Biospectrum-ABLE (Association of Biotechnology Led Enterprises), the Indian biotech industry passed the 4 Billion US$ mark in 2011-12, growing overall 15 percent compared to the previous year.

The Indian biotech industry has been booming over the past decade, growing from 0.5 Billion US$ in 2002-03 to more than 3.75 Billion US$ in 2010-11, and counting more than seven hundred players. As this includes the pharmaceutical sector with generics, the bioagri industry, bioindustrial applications, the bioinformatics area, equipment providers, and a wide range of bioservices, we felt the need for a better understanding of the potential of Indian biotech companies as actors or contributors to pharmaceutical Drug Discovery and Early Development. Our report summarizes our findings, based on more than two hundred and forty companies.

 

In the late nineteen eighties, Indian pharma companies started in-house drug discovery activities, aiming at developing the country’s first home-made drug. Pioneers like Ranbaxy and Dr Reddy’s were joined by companies like Glenmark, Biocon, Piramal, Sun, Torrent and Wockhardt. More recent players include Advinus, Zydus Cadila, Suven and a number of much smaller start-ups. Our report summarizes the current Drug Discovery and Development pipeline in India, with a total of more than ninety New Chemical Entities at various stages of (pre)clinical development.