Fighting Coronavirus - an update on Remdesivir

Fighting Coronavirus – an update on Remdesivir by Gilead

Posted 13 Apr 2020 by admin

Great to see the recent early clinical trial results for Remdesivir showing some benefit in a small study of hospitalised infected patients.⁽¹⁾

The results of larger more detailed trials will be eagerly awaited. If effective the need to supply significant amounts of this drug will be essential.

The synthesis of Remdesivir is a long linear process, although the cost per dose is relatively cheap. Gilead have made significant improvements to the manufacturing route, reducing it from one year to six months.⁽²⁾

If Remdesivir is shown to be effective in larger trials, the demand for the drug will significantly outstrip the ability to supply.

Gilead stated they currently have ~1.5 million doses available, which could provide ~140,000 treatment courses. As the global population is ~7 billion, then supply needs to be significantly increased.⁽³⁾

The drug was originally designed to be given as an intravenous infusion, meaning anyone receiving treatment would need this to happen in a suitably conducted environment.

In order to allow greater dosing to the general population, assessment of the ability to dose the drug orally, or via a more straightforward manner need to be looked into, as a matter of urgency. Reformulation or other dosing regimens might provide suitable alternatives.

As mentioned in our last post, it would be great to see the chemistry community working collaboratively to come up with alternative approaches that could impact supply of this and other potentially pivotal drugs in the fight to keep this virus contained.

References:

⁽¹⁾ Data on 53 Patients Treated With Investigational Antiviral Remdesivir Through the Compassionate Use Program Published in New England Journal of Medicine – https://www.gilead.com/news-and-press/press-room/press-releases/2020/4/data-on-53-patients-treated-with-investigational-antiviral-remdesivir-through-the-compassionate-use-program-published-in-new-england-journal-of-medici

⁽²⁾ Working to Supply Remdesivir for COVID-19 – https://www.gilead.com/purpose/advancing-global-health/covid-19/working-to-supply-remdesivir-for-covid-19

⁽³⁾ 1.5 Million Doses of Experimental Coronavirus Drug Remdesivir Donated by Biotech Firm Gilead – https://www.newsweek.com/15-million-doses-experimental-coronavirus-drug-remdesivir-donated-biotech-firm-gilead-1496247

Impacting COVID-19 – Opportunities for Chemists

Posted 25 Mar 2020 by admin

Dear Chemists,

We’re all aware of the situation we all are currently facing. We do these jobs for a love of chemistry and to steal a punchline from my old employer, making a meaningful difference to ~~patients~~ humanity.

Now is the time when we can openly collaborate to do our part and potentially protect many lives.

Gilead’s Remdesivir looks to be the most promising compound to help tackle COVID-19 in the short/medium term, along with a number of molecules that are in clinical development or repurposing of marketed drugs (including hydroxychloroquine, camostat etc., to name a few).

If any of these show positive effects, then supply will not be able to meet demand.

Remdesivir is patented and these will be active for many years. However, companies like Abbvie have already agreed to open up competition to its HIV med Kaletra (Aluvia).

I’m sure Gilead’s chemists have come up with robust routes for Remdesivir, but novel manufacturing routes will need to developed very rapidly, so the available chemical pool can be used as efficiently and innovatively as possible.

As a community that is used to innovating and solving problems, we can work openly and collaboratively, to provide rapid solutions.

From my reading of the literature the lactone below is a key intermediate in the synthesis of Remdesivir.

Further literature review shows the lactone can in turn be made from:

This bicycle is an interesting structure, but more importantly, it can be synthesised from lignocellulose, which is the most abundant and renewable biomass on earth. A number of chemistry groups have evaluated this process in the past, but conversion and yields still remain modest.

We have some of the greatest minds on the planet working across chemistry. Solving problems like these through open source discussions and experiments will undoubtedly put us in a stronger position over the coming months to increase the number of available treatment options and hopefully save many lives.

The o2h group supports early stage therapeutic companies through collaborative drug discovery research, investment and incubation, with teams in Cambridge, UK and Ahmedabad in India. We are prepared to help this cause in any way we can.

If plans can be rapidly collated, I’m sure governments across the world would see this effort as essential and allow chemical shipments and key research to be continued.

Let’s make sure when we look back in six months’ time we can be proud of our collective legacy and what we were able to deliver for ourselves, families, colleagues, friends and humanity.

Andy Morley

Chief Scientific Officer, o2h group

(Img source: https://news.ucr.edu/)

Nilesh Dagia, COO, o2h discovery, wins the International Institute for Sustainable Labs (I2SL) Go Beyond Award

Posted 13 Nov 2019 by admin

Colorado, USA, November 13 2019: We are absolutely delighted to announce that Nilesh Dagia, COO, o2h discovery, has won the Go Beyond Award in the Individual category at the 2019 I2SL Annual Conference. The Go Beyond award goes to the individual that demonstrated a commitment to advancing both science and sustainability, and their efforts to contribute to the overall goal of more efficient laboratories across the world.

Nilesh won the award for leading the design and execution of energy-efficient and environmentally responsible labs for o2h discovery in India. The Go Beyond Awards is a unique awards program honoring organizations, individuals, products and projects that are advancing sustainable, high-performance facilities.

On receiving the award, Nilesh Dagia said “I am thrilled and honored to have received the award from I2SL. A big thank you to my colleagues at o2h discovery as well as the entire design team for our upcoming state-of-the-art Shirish Research Center in India. It is important for us to put the latest thinking in sustainability into practice. We, at o2h discovery, continually work at analysing and reducing our carbon footprint and we have now set a goal to become carbon neutral. As a first step we shall plant 10,000 new trees.”

o2h group has visualised a home in the form of two iconic state-of-the-art research parks bridging India and Europe, and firmly taking a place alongside some of the most exciting innovation cultures and communities from around the world. The first of these research parks is being built on the recently acquired 2.76 acre heritage Hauxton Mill site in the UK, with plans to develop it into The Mill SciTech Park to create one of the region’s most exciting community of entrepreneurs in life-science, technology and social enterprise.

The second site is the Shirish Research Centre, Ahmedabad, India, a new purpose built research park, adjacent to the current o2h discovery site. The co-founders of the o2h group, Sunil and Prashant Shah wanted to create a truly inspiring home for research in India.

Editor Notes:

About I2SL

The International Institute for Sustainable Laboratories is a 501(c)(3) nonprofit organization dedicated to the design, engineering, and use of sustainable laboratories and other high-technology facilities worldwide. Through worldwide partnerships and the exchange of technical information, I2SL encourages the development of high-tech facilities that address the rapid pace of science, medicine, research, and development in an ever-changing and dynamic environment

The International Institute for Sustainable Laboratories (I2SL) is devoted to the principles of sustainable laboratories and related high-technology facilities, from design to engineering to operation. Each year, the I2SL Annual Conference highlights recent advancements in laboratory efficiency and performance, providing the laboratory and high-performance facility community with a unique forum for information exchange and education

For more information, please see www.i2sl.org

About o2h discovery:

Founded in 2005, o2h discovery has an integrated drug discovery platform operating from our research center in India and The Mill SciTech Park, Cambridge, UK. We have the in-house capability to execute hit-lead-optimization programs leading into patent and IND filing from our biotechnology incubator with expertise in discovery chemistry, biology, pharmacology and the on-going project management of pre-clinical development.

o2h discovery has developed and launched its proprietary application AI-Chemistry in the CloudTM which is the world’s first app to revolutionize the project management of external drug discovery programs. The app also enables communication between various scientific stakeholders essential for successful project advancement – leading to faster decision making.

For more information, please visit www.o2h.com

Media Contact:

Ajit Singh

Marketing Manager, o2h discovery

ajit@o2h.com

Therapeutics