Peptide Trends February 2021

Peptide Trends February 2021

February 28, 2021

Meet us at Asia Tides

TIDES Asia 2021 will take place on March 2 – 5 as a virtual webinar series presented in Japan Standard Time (JST). The Virtual Scientific Forum is free to attend and consists of 4 world-renowned keynote speakers and several cutting-edge technology company and CMO speakers who will present some of the latest R&D and CMC/manufacturing developments in the field.

Join our presentations on Day Two, Wednesday, March 3rd:

10:00am – 11:00am: Dr. Jyothi Thundimadathil, Associate Director, Bachem Americas, will present “Microspheres and Nanoparticles for Peptide Delivery”
11:00am – 12:00pm: Dr. Wolfgang Seufert, Director of Production, Bachem AG, will present “Solubility-directed Development of Trileucine Process”

Bachem‘s pipeline contains more than 150 customer projects in preclinical and clinical phases. In the last couple of years, a number of products in phase III trials received marketing authorization and phase II projects progressed to phase III clinical trials. In addition, Bachem is strategically diversifying its technology platform to include the manufacture of therapeutic oligonucleotides and nucleic-acid-based medicine. A full-service oligonucleotide manufacturing facility is being built at the headquarters in Bubendorf, Switzerland.

We kindly invite you to check the TIDES Asia Resources Center for additional Bachem content (e.g. our poster “A New Turn on Peptide Purification” or the video “Oligonucleotides @ Bachem”).

We look forward to e-connect with you at TIDES Asia 2021!

First defense against the spread of diseases

In Vitro Diagnostic Peptides

In vitro diagnostics are increasingly important around the world as a first defense against the spread of many diseases. They are defined as reagents, instruments, and systems intended for use in diagnosis of disease or other conditions, including a determination of the state of health, in order to cure, mitigate, treat, or prevent disease or its sequelae [1]. In vitro diagnostics have become essential and critical tools for medicine practice for diagnostics in order to rapidly detect with accuracy diseases and changes in drug resistance. Peptide-based in vitro diagnostics are used in particular for detection of infectious diseases, cardiac diseases, cancer and immune disorders. Peptides are major components of immunoassays, such as ELISA, Western blot, radioimmunoassay or ELISPOT that are used to measure the presence or concentration of a biomarker molecule. To make these tests accurate and to avoid false positive or negative results, the quality of the peptide is of high importance.

Our Center of Excellence for Custom Synthesis in St. Helens (UK) is certified according to ISO 13485 for the manufacture of peptides as critical raw materials for medical devices. It offers a state-of-the-art quality management system and peptide manufacturing equipment. Additional services such as the use of dedicated equipment during manufacturing and customized vialing of the finished product are available.

At Bachem, we assist our partners at every stage of product development: from early stage R&D all the way through to commercialization. We provide peptides from research use, clinical development to API production. Together with our clients, we define the requirements (e.g. specifications, quality, dedicated equipment) and establish a robust manufacturing process for future commercial supply.

Quality you can trust

Regulatory requirements and standards in documentation and change control for in the in vitro diagnostic industry are constantly evolving. Bachem’s Research Grade Plus (RGP) service has been established for our customers with additional quality requirements that can be adapted «à la carte» to meet your specific needs (see table below).

Benefits of the Bachem Research Grade Plus

Research Grade Plus guarantees full traceability of critical raw materials throughout the whole supply chain, manufacturing according to an established and robust process, as well as batch-to-batch consistency for your peptides.

We set industry standards for high quality custom peptides. Our high capacity and state-of-the-art production equipment are dedicated to yield your peptide in the quality and purity you require. Further, we offer you our experienced technical support that will help you to identify the additional services that best suit your requirements.

 

Chemistry & Quality

  • SPPS including a large selection of modifications
  • State-of-the-art manufacturing & analytical capabilities

Capacity

  • From mg up to 100g production scale
  • Parallel production of multiple peptides

Dispensing

  • Manual and fully automated dispensing capabilities
  • Experienced in peptide mixture preparation

Support

  • Stability study
  • MDF (Medical Device File)

 

For more details on In Vitro Diagnostics at Bachem and our Custom Synthesis service, please consult our new brochure and our website.

 

References

[1] Source FDA

Advancing through 2020: Peptide drug approvals

The year 2020 brought positive developments in the form of approved drug applications for peptides. The U.S. Food and Drug Administration (FDA) approved Rhythm Pharmaceuticals’ Imcivree (setmelanotide), a novel peptide-based drug for the treatment of obesity and the control of hunger associated with pro-opiomelanocortin deficiency. In Europe, the European Medicines Agency (EMA) granted conditional approval to MYR Pharmaceuticals’ Hepcludex (bulevirtide) for the treatment of Hepatitis D virus (HDV) infection. In addition, drugs with leuprolide, octreotide and vasopressin as active pharmaceutical ingredients were among the approved Abbreviated New Drug Applications (ANDA) and 505(b)[2] applications [1].

 

Novel Therapeutic Peptide Drug Approvals

As noted, two novel therapeutic peptide drugs, Imcivree and Hepcludex, each received approval from a major drug regulatory authority in 2020. Both peptides were designated orphan drugs by the FDA and EMA and received additional designations designed to facilitate development or expedite the review of their marketing applications.

Imcivree (setmelanotide), approved in November 2020, is a novel peptide drug developed for chronic weight management in patients with obesity due to three rare genetic conditions including pro-opiomelanocortin (POMC) deficiency, proprotein subtilisin/kexin type 1 (PCSK1) deficiency, and leptin receptor (LEPR) deficiency. 

Figure 1 Structure of setmelanotide (Source: FDA)

The FDA designated Imcivree as a breakthrough therapy, a special program designed to shorten the development time of potentially important new drugs for serious or life-threatening diseases. The FDA also granted the drug Priority Review and Orphan Drug designation [1]. For the European market, Rhythm Pharmaceuticals has already submitted a Marketing Authorization Application to the EMA for setmelanotide to treat people with obesity due to POMC, PCSK1 or LEPR deficiency. This application is currently under review

Hepcludex (bulevirtide) is an antiviral peptide-based drug used to treat chronic hepatitis D virus (HDV) infection, the most severe form of hepatitis, in adults with compensated liver disease. The peptide is composed of a 47-amino acid sequence derived from the N-terminal domain of the hepatitis B virus (HBV) surface protein with an N-terminal myristoyl moiety [2].

Figure 2 Structure of bulevirtide (Source: EMA)

In July 2020, the European Commission granted Conditional Marketing Authorization (CMA) for Hepcludex for the treatment of chronic hepatitis D virus infection making it the first therapy approved for hepatitis D. The approval of Hepcludex was based on results from two Phase 2 studies, which demonstrated a beneficial effect of Hepcludex in patients with HDV infection as well as good tolerability and safety. In Europe, Hepcludex received Orphan Drug designation and PRIority Medicines (PRIME) scheme eligibility. Myr Pharmaceuticals is looking to expand access to Hepcludex in additional markets including the US. In the US, the FDA has already designated Hepcludex as a Breakthrough Therapy and Orphan Drug [3]. The company plans to file for accelerated approval in the US during the second half of 2021 [4].

Conclusion

Despite the intense global focus on COVID-19 and challenges associated with the pandemic, the pharmaceutical industry and regulatory authorities kept up the pace and advanced new peptide-based drugs for patients. As a peptide manufacturer, Bachem supports the pharmaceutical industry with the cGMP manufacturing of active pharmaceutical ingredients for clinical trials, product launch and commercialization. Bachem has approximately 50 years of experience in the development, production and filing of peptide active pharmaceutical ingredients.

 

References

[1] New Drug Therapy Approvals 2020. U.S. Food and Drug Administration 2021.

[2] Mechanism of Action. Myr Pharmaceuticals 2021.

[3] GlobalData 2021.

[4] Gilead Sciences to Acquire MYR GmbH. Gilead 2020.

Meet Bachem: Philippe Theron

What is your official job title at Bachem?

My official job title is Sales Manager Custom Synthesis.

How long have you been with Bachem? Where did you work before Bachem?

I joined Bachem mid-June 2020. Before, I worked in technical Sales in another CRO near Basel and over 10 years in Sales in a company producing industrial gases for labs in Switzerland.

Briefly, what do you do at Bachem?

I am in Sales for Custom Synthesis and Amino Acid Derivatives, but both activities are in the same team. I am in contact with customers mostly in Europe and Asia for scientific, commercial and administrative support.

What is your academic background/degrees or training?

I am a chemical engineer with a specialization in analytical chemistry. Moreover, I have a long experience in technical sales in several chemical and pharmaceutical Swiss companies. I also like to use my language skills, (Swiss)-German, French and English in my daily work.

What do you like to do outside of work (interests, hobbies)?

I am fond of sports, particularly road cycling and tennis. The Jura and Black Forest mountains are very nice spots to rediscover regularly. I am also a numismatist, collecting coins from all over the world. And I like to spend time in my garden with my family and friends.

What makes a perfect day for you?

At work, I like to support customers in their projects and it satisfies me if we move forward projects together. Of course, a nice commercial success is always a great motivation to continue to build up the business. And some free time to spend outside at during a sunny day is always nice.

What do you like most about your job?

I like to be considered as a technical and a scientific support for customers. But the most positive thing is to win new interesting projects and new customers for the long term in a sustainable way.

What do you do for fun?

I like to grow tomato plants from seedlings to juicy tomatoes in my garden. It takes some time compared to buying them in a supermarket, but I am always astonished to see what a seed can do in a few months’ time.

What is your preferred peptide?

That is a funny question! I cannot tell for peptides, but for amino acids, the preferred one is Threonine (Thr) as the beginning is written nearly like my name.

M.M.Edwards et al.

Chronic hindbrain administration of oxytocin elicits weight loss in male diet-induced obese mice.

American Journal of Physiology-Regulatory, Integrative and Comparative Physiology (2021)

 

M.D.Ericson et al.

Discovery of molecular Interactions of the human melanocortin-4 receptor (hMC4R) Asp189 (D189) amino acid with the endogenous G-protein-coupled receptor (GPCR) antagonist agouti-related protein (AGRP) provides insights to AGRP’s inverse agonist pharmacology at the hMC4R.

ACS Chemical Neuroscience 12, 542-556 (2021)

 

E.A.Wilson et al.

Gqα/G11α deficiency in dorsomedial hypothalamus leads to obesity resulting from decreased energy expenditure and impaired sympathetic nerve activity.

American Journal of Physiology-Endocrinology and Metabolism 320, E270-E280 (2021)

 

V.C.Can et al.

Novel anti-inflammatory and chondroprotective effects of the human melanocortin MC1 receptor agonist BMS-470539 dihydrochloride and human melanocortin MC3 receptor agonist PG-990 on lipopolysaccharide activated chondrocytes.

European Journal of Pharmacology 872, 172971 (2020)