Month: September 2021

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Drug Approvals 2021

Drug Approvals 2021

Published on 13-Sept-2021

In 2021, the FDA has approved many novel products that serve previously unmet medical needs or significantly help to advance patient quality of life. The broad indication wise distribution of all CDER’s 2021 drug approvals indicates notable advances in drug discovery1,2.

New Drug Approvals & Drugs in Pipeline (FDA) for 2021*

Table 1. Approved Drug List
Table 2. Drugs in Pipeline

*This information is updated as July 31, 2021; listed alphabetically by trade name.

Significant drug launches of 2021

  • Verquvo (Vericiguat, MERCK SHARP DOHME, 01/19/2021)
    Mitigates the risk of cardiovascular death and hospitalization for chronic heart failure 
  • Cabenuva (Cabotegravir and Rilpivirine (Co-Packaged), VIIV HLTHCARE, 01/21/2021)
    Treats HIV 
  • Lupkynis (Voclosporin, AURINIA, 01/22/2021)
    Treats lupus nephritis 
  • Tepmetko (Tepotinib, EMD SERONO INC, 02/03/2021)
    Treats non-small cell lung cancer 
  • Ukoniq (Umbralisib Tosylate, TG THERAPS, 02/05/2021) 
    Treats marginal zone lymphoma and follicular lymphoma 
  • Evkeeza (Evinacumab-Dgnb, REGENERON PHARMACEUTICALS, 02/11/2021) 
    Treats homozygous familial hypercholesterolemia
  • Cosela (Trilacicilib Dihydrochloride, G1 THERAP, 02/12/2021), 
    Mitigates chemotherapy-induced myelosuppression in small cell lung cancer
  • Amondys 45 (Casimersen, SAREPTA THERAPS INC, 02/25/2021)
    Treats Duchenne muscular dystrophy
  • Nulibry (Fosdenopterin Hydrobromide, ORIGIN, 02/26/2021) 
    Reduces the risk of mortality in molybdenum cofactor deficiency Type A 
  • Pepaxto (Melphalan Flufenamide Hydrochloride, ONCOPEPTIDES AB, 02/26/2021)
    Treats relapsed or refractory multiple myeloma 
  • Azstarys (Serdexmethylphenidate Hydrochloride; Dexmethylphenidate Chloride, COMMAVE THERAP, 03/02/2021)
    Treats attention deficit hyperactivity disorder 
  • Fotivda (Tivozanib Hydrochloride, AVEO PHARMS, 03/10/2021)
    Treats renal cell carcinoma 
  • Ponvory (Ponesimod, JANSSEN PHARMS, 03/18/2021)
    Treats relapsing forms of multiple sclerosis
  • Zegalogue (Dasiglucagon Hydrochloride, ZEALAND PHARMA, 03/22/2021)
    Treats severe hypoglycemia 
  • Qelbree (Viloxazine Hydrochloride, SUPERNUS PHARMS, 04/02/2021)
    Treats attention deficit hyperactivity disorder 
  • Nextstellis (Drospirenone; Estetrol, MAYNE PHARMA, 04/15/2021)
    Prevents pregnancy 
  • Jemperli (Dostarlimab-Gxly, GLAXOSMITHKLINE, 04/22/2021)
    Treats endometrial cancer 
  • Zynlonta (Loncastuximab Tesirine-Lpyl, ADC Therapeutics SA, 04/23/2021)
    Treats certain types of relapsed or refractory large B-cell lymphoma 
  • Empaveli (Pegcetacoplan, APELLIS PHARMS, 05/14/2021)
    Treats paroxysmal nocturnal hemoglobinuria 
  • Rybrevant (Amivantamab-Vmjw, JANSSEN BIOTECH, 05/21/2021)
    Treats a subset of non-small cell lung cancer 
  • Pylarify (Piflufolastat F-18, PROGENICS PHARMS INC, 05/26/2021)
    Identifies prostate-specific membrane antigen-positive lesions in prostate cancer 
  • Lumakras (Sotorasib SIB, AMGEN INC, 05/28/2021)
    Treats types of non-small cell lung cancer 
  • Truseltiq (Infigratinib Phosphate, QED THERAP, 05/28/2021)
    Treats cholangiocarcinoma whose disease meets certain criteria
  • Lybalvi (Olanzapine; Samidorphan L-Malate, ALKERMES INC, 05/28/2021)
    Treats schizophrenia and certain aspects of bipolar I disorder
  • Brexafemme (Ibrexafungerp Citrate, SCYNEXIS, 06/01/2021)
    Treats vulvovaginal candidiasis
  • Aduhelm (Aducanumab-Avwa, BIOGEN INC, 06/07/2021)
    Treats Alzheimer’s disease 
  • Rylaze (Asparaginase Erwinia Chrysanthemi (Recombinant)-Rywn, JAZZ PHARMS, 06/30/2021)
    Treats acute lymphoblastic leukemia and lymphoblastic lymphoma in patients who are allergic to E. coli-derived asparaginase products, as a component of a chemotherapy regimen 
  • Kerendia (Finerenone, BAYER HEALTHCARE PHARMACEUTICALS INC, 07/09/2021)
    Reduces the risk of kidney and heart complications in chronic kidney disease associated with type 2 diabetes 
  • Fexinidazole (Fexinidazole, DNDI, 07/16/2021)
    Treats human African trypanosomiasis caused by the parasite Trypanosoma brucei gambiense 
  • Rezurock (Belumosudil, KADMON PHARMS LLC, 07/16/2021)
    Treats chronic graft-versus-host disease after failure of at least two prior lines of systemic therapy
  • Bylvay (Odevixibat, ALBIREO PHARMA INC, 07/20/2021)
    Treats pruritus 
  • Twyneo (Tretinoin and benzoyl peroxide, SOL-GEL TECHNOLOGIES LTD, 07/26/2021)
    It is a topical retinoid and antibacterial fixed-dose combination for the treatment of acne vulgaris in adults and children 9 years of age and older
  • Saphnelo (Anifrolumab, AstraZeneca, 07/30/2021)
    It is a type I interferon (IFN) receptor antagonist indicated for the treatment of adult patients with moderate to severe systemic lupus erythematosus (SLE), who are receiving standard therapy 

Significant Drug launches in Pipeline for 2021

  • Oteseconazole (VT-1161, MYCOVIA PHARMACEUTICALS INC)
    It is an investigational oral antifungal in development for the treatment of recurrent vulvovaginal candidiasis (RVVC)
  • Sulopenem (ITERUM THERAPEUTICS PLC)
    It is an orally bioavailable, broad-spectrum penem β-lactam antibiotic in development for the treatment of infections caused by multi-drug resistant bacteria
  • Brixadi (Buprenorphine, BRAEBURN INC)
    It is a long-acting partial opioid agonist injection formulation in development for the treatment of opioid use disorder
  • Tenapanor (ARDELYX INC)
    It is a sodium/hydrogen exchanger 3 (NHE3) inhibitor in development for the control of serum phosphorus in adult patients with chronic kidney disease (CKD) on dialysis or Hyperphosphatemia of Renal Failure
  • Libervant (Diazepam, AQUESTIVE THERAPEUTICS INC)
    It is a buccal film formulation of the approved benzodiazepine diazepam in development for the management of seizure clusters
  • Roxadustat (FG-4592, FIBROGEN INC)
    It is a first-in-class, orally administered small molecule hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anaemia of chronic kidney disease (CKD)
  • Tezepelumab (AMGEN AND ASTRAZENECA)
    It is an investigational, potential first-in-class anti-thymic stromal lymphopoietin (TSLP) monoclonal antibody in development for the treatment of severe asthma
  • LV-101 (Carbetocin intranasal, LEVO THERAPEUTICS INC)
    It is an oxytocin analog in development as a treatment for hyperphagia and behavioral distress associated with Prader-Willi syndrome (PWS)
  • Teplizumab (PROVENTION BIO INC)
    It is an investigational anti-CD3 monoclonal antibody (mAb) in development for the delay or prevention of clinical type 1 diabetes (T1D) in at-risk individuals
  • Surufatinib (HUTCHISON CHINA MEDITECH LIMITED)
    It is a novel, oral angio-immuno kinase inhibitor in development for the treatment of pancreatic and non-pancreatic neuroendocrine tumors (“NET”)
  • Lenacapavir (GILEAD SCIENCES INC)
    It is an investigational, long-acting HIV-1 capsid inhibitor in development for the treatment of HIV-1 infection in heavily treatment-experienced (HTE) people with multi-drug resistant (MDR) HIV-1 infection
  • Vutrisiran (ALNYLAM PHARMACEUTICALS INC)
    It is an investigational RNAi therapeutic in development for the treatment of the polyneuropathy of hereditary transthyretin-mediated (hATTR) amyloidosis in adults
  • Pedmark (Sodium thiosulfate, FENNEC PHARMACEUTICALS INC)
    It is a cisplatin neutralizing agent in development for the protection against hearing loss in pediatric patients receiving cisplatin chemotherapy
  • Mitapivat (AGIOS PHARMACEUTICALS, INC)
    It is a protein kinase-R (PKR) activator in development for the treatment of adults with pyruvate kinase (PK) deficiency
  • Arimoclomol (ORPHAZYME A/S)
    It is an investigational Heat-Shock Protein amplifier in development for the treatment of Niemann-Pick disease Type C (NPC)
  • Ruxolitinib (INCYTE DERMATOLOGY)
    It is a JAK1/JAK2 inhibitor formulated for topical application in development for the treatment of atopic dermatitis and vitiligo
  • Zimhi (Naloxone hydrochloride, ADAMIS PHARMACEUTICALS CORPORATION)
    It is a high-dose formulation of the approved opioid antagonist naloxone in development for the treatment of opioid overdose
  • Tapinarof (DERMAVANT SCIENCES)
    It is a topical aryl hydrocarbon receptor (AhR) modulating agent in development for the treatment of plaque psoriasis and atopic dermatitis
  • Plinabulin (BEYONDSPRING INC)
    It is a selective immunomodulating microtubule-binding agent (SIMBA) in development for use in combination with granulocyte colony-stimulating factor (G-CSF) for the prevention of chemotherapy-induced neutropenia (CIN)

References

  1. US FDA
  2. Drugs.com
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GOSTAR CONTENT UPDATES – 2021

GOSTAR Content Updates - 2021

Published on 13-Sept-2021

GOSTAR is the largest manually annotated structure-activity relationships (SAR) database of small molecules published in mainstream medicinal chemistry journals and patents. Compounds from both discovery and development stages targeting all target families are covered. Along with SAR, key properties like ADME, and Toxicity are captured. This relational database enables users to navigate and analyze the massive content of small molecules to derive insightful decisions in the design and discovery of novel compounds.

Content Coverage

The GOSTAR database is composed of many different types of content, from the scientific literature to publicly available material.

  • MedChem Journals
  • Patents
  • FDA/EMEA/PMDA Reports
  • Clinical Trial Registries
  • Scientific Reviews
  • Company websites
  • Books
  • Conferences
  • Public Sources
Fig 1. A quick view of content covered and sources of the content

Preclinical Candidates Covered in 2021 (until July’2021)

In the year 2021, the GOSTAR database is enriched with various preclinical compounds acting against various indications like COVID-19, Non-alcoholic steatohepatitis (NASH), Hepatitis virus infections, HIV infections, Cardiovascular diseases, and various cancers.

Few significant drug inclusions until July 31, 2021: 

  • Synflorix
  • AZD1222
  • Benaglutide
  • GSK-1557484A
  • MRNA-1273

Target Space Covered in 2021 Updates

 

New content is updated for more than 2400 protein targets into the GOSTAR database until July 31, 2021.

Table 2: List of top 20 targets covered

Type of Content

Further deep analysis of the content covered in 2021 is shown in figure 2. Of the 1.2 million SAR rows added to GOSTAR, functional in-vitro and in-vivo contribute 41% to data, binding constitutes 33%, and 5% of content consists of ADME properties. 2% of content covers toxicity properties of compounds covered in 2021 and the rest 19% represents other property types including physicochemical properties.

Fig 2. Assay wise distribution of SAR content
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Biologics – The Biotech Drugs Transforming Medicine

Biologics - The Biotech Drugs Transforming Medicine

Published on 13-Sept-2021

Biologics, also known as biological products, are any type of medicines derived from living organisms such as humans, animals, or microorganisms via highly complex manufacturing processes and administered under closely monitored conditions. This is in contrasts to traditional non-biologic pharmaceutical drugs, which are synthesized in a laboratory through chemical processes without the use of components of living matter. Cancer, infectious diseases, autoimmune disease are among the ailments for which biologics are used to prevent, treat, or cure (Fig. 1).

Figure 1. Biologic medicines in development by therapeutic category [1].

Note: Some medicines are being explored in more than one therapeutic category.

Biologics include a wide variety of products such as monoclonal antibodies, vaccines, gene and cell therapies, and recombinant proteins (Fig. 2).

Figure 2. Biologic medicines in development by product category [1].

Monoclonal antibodies are by far the most researched category of biologics with at least 338 therapeutic mAbs currently being developed by pharmaceutical companies [1].

Monoclonal antibody (mAb) – the bestselling category of biological products.

Antibody engineering has significantly advanced ever since the approval of the first monoclonal antibody by the United States Food and Drug Administration (US FDA) in 1986 [2]. Therapeutic antibodies currently available in the market are safe with fewer adverse effects owing to their high specificity. Consequently, antibody drugs have become the leading class of newly developed drugs in recent years. Eight of the top ten bestselling drugs worldwide in 2018 were biologics. In 2018, the global therapeutic monoclonal antibody was worth roughly US$115.2 billion, with revenues expected to reach $300 billion by 2025 (Fig. 3) [3].

Figure 3. Timeline from 1975 showing the successful development of therapeutic antibodies and their applications [3].

As of December 2019, US FDA had approved 79 therapeutic mAbs, including 30 for cancer treatment [4].

Best-selling biotech drugs worldwide

AbbVie’s Humira and Merck’s Keytruda are among the top-selling biotechnology drugs in the world, generating 19.6 billion and 11.1 billion U.S. dollars, respectively, in 2019 (Fig. 4) [5]. Oncology, autoimmune/immunology, hematology, ophthalmology, and dermatology are among the top five therapy areas in 2019. Oncologic treatments account for six of the top-selling drugs in 2019, making oncology the most targeted field [6].

Figure 4. Top selling biotech drugs worldwide in 2019 [6].

Bristol Myers Squibb, AbbVie, Pfizer, and Roche are four pharmaceutical companies with more than one best-selling drug of 2019. Bristol Myers Squibb had the most top-selling drugs (Eliquis, Opdivo, and Revlimid) in 2019, accounting for 63% of the company’s total revenue. Whereas AbbVie’s revenues in 2019 were significantly reliant on its main products (Humira and Imbruvica), which accounted for 72% of the company’s total revenues [6]. The United States spent approximately 45 billion U.S. dollars on biotechnology research and development. In addition, the United States had approximately 34% of the world’s share of biotechnology patents filed in 2014, while Germany filed 8% of global biotech patents [5].

The Rise of Biosimilars

A biosimilar is a biologic that is similar to another biologic medicine (known as a reference product) that has already been approved by the FDA in the United States. In terms of safety, purity, and potency, biosimilars are very similar to the reference product, but there may be minor differences in clinically inactive components. The biologics and biosimilars industry in the United States is fast expanding, and as new medications are introduced, the benefits for patient access and cost management will continue to grow. There are 18 biosimilars on the market in the United States as of November 2020, competing against seven reference biologics, with ten more FDA-approved biosimilars expected to hit the market in the coming years [7].

Biosimilars save money in the long run, with higher savings coming from newer launches competing against more expensive drugs. The gap between the originator and the mean Average Sales Price (ASP) of their biosimilars ranged from 8.1 percent to 45.1 percent lower than the originator products as of July 2020 (including insulins) [7]. Biosimilars saved 6.5 billion U.S. dollars annually in the second quarter of 2020, and savings are expected to exceed 100 billion U.S. dollars over the next five years [8].

A biopharmaceutical product knowledge base is the need of the hour

Antibodies are the most successful class of biotherapeutics because of their binding versatility [9]. With the rapid growth of therapeutic antibody research, the chances of a specific antibody being the only one against a certain antigen are decreasing. Understanding the methods used to produce competing antibodies, as well as their pros and cons, can be extremely helpful in moving therapeutic antibodies forward. Data from clinical trials dominate the scientific literature on therapeutic antibodies, rather than the details of pre-clinical development that is underway for nearly two-thirds of all therapeutic antibodies. The information on the latter could only be obtained from patents. Many researchers are put off by patents’ opaque and archaic language but hidden in the text of these files are details about antibody sequences, assay techniques, epitopes, and much more. Patent applications are usually the first public disclosure of novel antibodies, often months or even years before conference papers or clinical trials. Researchers can identify novel antibodies in early stages of development months or years before they are formally announced by mining the patent literature.

There are very few databases that harvest this information. The IMGT Monoclonal Antibody Database and WHOINNIG are two non-commercial resources for antibody research. Other databases that aren’t unique to antibodies, such as ChEMBL, DrugBank, and KEGG DRUG, also capture WHO data. Most databases deliver additional metadata for their therapeutic entries, such as clinical trial status, companies involved in the development, target specificity, and alternative names. While these archives include sequence information, it is currently not possible to query them by sequence or to bulk-download relevant collections of therapeutic sequences for direct bioinformatic analysis.

Excelra is strongly positioned to deliver tailor-made curation on chemically defined antibodies (i.e., antibodies with a known primary amino-acid sequence) connected with their antigenic target, which can be either a protein or a chemical entity.

For more information and to connect with our scientific teams, write to us on: marketing@excelra.com

References

  1. PhRMA [Pharmaceutical Research and Manufacturers of America] (2013). Medicines in Development: Biologics. 2013 Report. http://www.phrma.org/sites/default/files/pdf/biologics2013.pdf Accessed 10 Jul 2021.
  2. Ecker, D. M., Jones, S. D., Levine, H. L. The therapeutic monoclonal antibody market. MAbs. 2015, 7, 9–14.
  3. Lu, R. M., Hwang, Y. C., Liu, I. J. et al.Development of therapeutic antibodies for the treatment of diseases. J Biomed Sci. 2020, 27 (1), 1-30.
  4. The Antibody Society (2019). In: Approved antibodies. https://www.antibodysociety.org Accessed 10 Jul 2021.
  5. Statistica (2020). Select top selling biotech drugs worldwide in 2019. https://www.statista.com/statistics/299138/top-selling-biotech-drugs-based-on-revenue/ Accessed 10 Jul 2021.
  6. PharmaIntelligence (2020). Top 10 Best-Selling Drugs of 2019. https://pharmaintelligence.informa.com/~/media/informa-shop-window/pharma/2020/files/reports/top-10-best-selling-drugs-of-2019.pdf Accessed 10 Jul 2021.
  7. IQVIA Institute Report (2020). Biosimilars in the United States 2020 – 2024. https://www.iqvia.com/-/media/iqvia/pdfs/institute-reports/iqvia-institute-biosimilars-in-the-united-states.pdf?_=1606843358393 Accessed 10 Jul 2021.
  8. IQVIA Institute Report (2020). Biosimilars in the United States 2020 – 2024. https://www.iqvia.com/-/media/iqvia/pdfs/institute-reports/iqvia-institute-biosimilars-in-the-united-states.pdf?_=1606843358393 Accessed 10 Jul 2021.
  9. Kaplon, H., Muralidharan, M., Schneider, Z., Reichert, J. M. Antibodies to watch in 2020. MAbs. 2020, 12(1), 1703531.