scholarly journals The Pharmaceutical Industry in 2019. An Analysis of FDA Drug Approvals from the Perspective of Molecules

Molecules ◽  
2020 ◽  
Vol 25 (3) ◽  
pp. 745 ◽  
Author(s):  
Beatriz G. de la Torre ◽  
Fernando Albericio
Keyword(s):  
Natural Products ◽  
Pharmaceutical Industry ◽  
Small Molecules ◽  
Chemical Structure ◽  
New Drugs ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
The Us ◽  
New Chemical Entities ◽  
Antibody Drug

During 2019, the US Food and Drug Administration (FDA) approved 48 new drugs (38 New Chemical Entities and 10 Biologics). Although this figure is slightly lower than that registered in 2018 (59 divided between 42 New Chemical Entities and 17 Biologics), a year that broke a record with respect to new drugs approved by this agency, it builds on the trend initiated in 2017, when 46 drugs were approved. Of note, three antibody drug conjugates, three peptides, and two oligonucleotides were approved in 2019. This report analyzes the 48 new drugs of the class of 2019 from a strictly chemical perspective. The classification, which was carried out on the basis of chemical structure, includes the following: Biologics (antibody drug conjugates, antibodies, and proteins); TIDES (peptide and oligonucleotides); drug combinations; natural products; and small molecules.

scholarly journals The Pharmaceutical Industry in 2020. An Analysis of FDA Drug Approvals from the Perspective of Molecules

Molecules ◽  
2021 ◽  
Vol 26 (3) ◽  
pp. 627 ◽  
Author(s):  
Beatriz G. de la Torre ◽  
Fernando Albericio
Keyword(s):  
Pharmaceutical Industry ◽  
Small Molecules ◽  
New Drugs ◽  
Biologic Drugs ◽  
Antibody Drug Conjugates ◽  
Aromatic Heterocycles ◽  
Drug Conjugates ◽  
New Chemical Entities ◽  
Pharmaceutical Agents ◽  
Antibody Drug

Although the pharmaceutical industry will remember 2020 as the year of COVID-19, it is important to highlight that this year has been the second-best—together with 1996—in terms of the number of drugs accepted by the US Food and Drug Administration (FDA). Each of these two years witnessed the authorization of 53 drugs—a number surpassed only in 2018 with 59 pharmaceutical agents. The 53 approvals in 2020 are divided between 40 new chemical entities and 13 biologic drugs (biologics). Of note, ten monoclonal antibodies, two antibody–drug conjugates, three peptides, and two oligonucleotides have been approved in 2020. Close inspection of the so-called small molecules reveals the significant presence of fluorine atoms and/or nitrogen aromatic heterocycles. This report analyzes the 53 new drugs of the 2020 harvest from a strictly chemical perspective, as it did for those authorized in the previous four years. On the basis of chemical structure alone, the drugs that received approval in 2020 are classified as the following: biologics (antibodies, antibody-drug conjugates, and proteins); TIDES (peptide and oligonucleotides); natural products; fluorine-containing molecules; nitrogen aromatic heterocycles; and other small molecules.

scholarly journals The Pharmaceutical Industry in 2018. An Analysis of FDA Drug Approvals from the Perspective of Molecules

Molecules ◽  
2019 ◽  
Vol 24 (4) ◽  
pp. 809 ◽  
Author(s):  
Beatriz G. de la Torre ◽  
Fernando Albericio
Keyword(s):  
Natural Products ◽  
Pharmaceutical Industry ◽  
Small Molecules ◽  
Drug Administration ◽  
Chemical Structure ◽  
Food And Drug Administration ◽  
New Drugs ◽  
Previous Record ◽  
New Chemical Entities ◽  
Important Milestone

The Food and Drug Administration approved 59 new drugs (42 New Chemical Entities and 17 Biologics) during 2018. This number breaks the previous record of 53 approved by the same organization in 1996. The 17 new biologics approved in 2018 also represent an important milestone for this kind of drug and they clearly exceed the 12 approved in 2015 and 2017. Herein, the 59 new drugs of the class of 2018 are analyzed from a strictly chemical perspective. The classification has been carried out on the basis of the chemical structure and includes the following: Biologics (antibodies and enzymes); TIDES (peptides and oligonucleotides) and natural products; drug combinations; and small molecules.

scholarly journals 2019 FDA TIDES (Peptides and Oligonucleotides) Harvest

2020 ◽  
Vol 13 (3) ◽  
pp. 40 ◽  
Author(s):  
Danah Al Shaer ◽  
Othman Al Musaimi ◽  
Fernando Albericio ◽  
Beatriz G. de la Torre
Keyword(s):  
Adverse Effects ◽  
Mode Of Action ◽  
Chemical Structure ◽  
Imaging Agents ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Target Mode ◽  
Medical Indications ◽  
Antibody Drug ◽  
The Way

2019 has been an excellent year in terms of peptides and oligonucleotides (TIDES) approved by the FDA. Despite the drop in the number of total drugs approved by the FDA in 2019 in comparison with 2018 (48 vs. 59), the total number of TIDES authorized increased (seven vs. three). Year after year, TIDES are increasingly present in therapy, as imaging agents, theragnostic and constituent moieties of other complex drugs, such as antibody drug conjugates. This means a consolidation of these kinds of drugs in the pharmaceutical arena, paving the way in the coming years for the approval of others for diverse medical indications. Here the TIDES approved in 2019 are analyzed in terms of chemical structure, medical target, mode of action, and adverse effects.

scholarly journals Catalytic Cleavage of Disulfide Bonds in Small Molecules and Linkers of Antibody–Drug Conjugates

2019 ◽  
Vol 47 (10) ◽  
pp. 1156-1163 ◽  
Author(s):  
Donglu Zhang ◽  
Aimee Fourie-O’Donohue ◽  
Peter S. Dragovich ◽  
Thomas H. Pillow ◽  
Jack D. Sadowsky ◽  
...  
Keyword(s):  
Small Molecules ◽  
Disulfide Bonds ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Catalytic Cleavage ◽  
Antibody Drug

scholarly journals Challenges and opportunities to develop enediyne natural products as payloads for antibody-drug conjugates

2021 ◽  
Vol 4 (1) ◽  
pp. 1-15
Author(s):  
Ajeeth Adhikari ◽  
Ben Shen ◽  
Christoph Rader
Keyword(s):  
Natural Products ◽  
First Generation ◽  
Gemtuzumab Ozogamicin ◽  
Antibody Drug Conjugates ◽  
Clinical Utilization ◽  
Drug Conjugates ◽  
Dna Damaging Agents ◽  
Challenges And Opportunities ◽  
Antibody Drug

Abstract Calicheamicin, the payload of the antibody-drug-conjugates (ADCs) gemtuzumab ozogamicin (Mylotarg®) and inotuzumab ozogamicin (Besponsa®), belongs to the class of enediyne natural products. Since the isolation and structural determination of the neocarzinostatin chromophore in 1985, the enediynes have attracted considerable attention for their value as DNA damaging agents in cancer chemotherapy. Due to their non-discriminatory cytotoxicity towards both cancer and healthy cells, the clinical utilization of enediyne natural products relies on conjugation to an appropriate delivery system, such as an antibody. Here, we review the current landscape of enediynes as payloads of first-generation and next-generation ADCs.

scholarly journals Perspectives on the development of antibody-drug conjugates targeting ROR1 for hematological and solid cancers

2021 ◽  
Author(s):  
Haiyong Peng
Keyword(s):  
Cancer Therapy ◽  
Small Molecules ◽  
Pharmaceutical Companies ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Solid Malignancies ◽  
Selective Delivery ◽  
And Performance ◽  
Antibody Drug ◽  
Made In

Abstract Antibody–drug conjugates (ADCs) are targeted therapeutics generated by conjugation of cytotoxic small molecules to monoclonal antibodies (mAbs) via chemical linkers. Due to their selective delivery of toxic payloads to antigen-positive cancer cells, ADCs demonstrate wider therapeutic indexes compared to conventional chemotherapy. After decades of intensive research and development, significant advances have been made in the field, leading to a total of ten FDA-approved ADCs to treat cancer patients. Currently, ~ 80 ADCs targeting different antigens are under clinical evaluation for treatment of either hematological or solid malignancies. Notably, 3 ADCs targeting the same oncofetal protein, ROR1, have attracted considerable attention when they were acquired or licensed successively in the fourth quarter of 2020 by 3 major pharmaceutical companies. Apparently, ROR1 has emerged as an attractive target for cancer therapy. Since all the components of ADCs, including the antibody, linker, and payload, as well as the conjugation method, play critical roles in ADC’s efficacy and performance, their choice and combination will determine how far they can be advanced. This review summarizes the design and development of current anti-ROR1 ADCs and highlights an emerging trend to target ROR1 for cancer therapy.

Antibody–Drug Conjugates in Relapsed/Refractory CD30-positive Lymphomas

2015 ◽  
Vol 11 (2) ◽  
pp. 123
Author(s):  
Ulrich Jager ◽  
Martin Hutchings ◽  
◽  
Keyword(s):  
Large Cell ◽  
Brentuximab Vedotin ◽  
Phase Ii Trials ◽  
Two Phase ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
The Us ◽  
Accelerated Approval ◽  
Cluster Of Differentiation ◽  
Antibody Drug

Although chemotherapy and radiotherapy are associated with good outcomes in patients with advanced Hodgkin’s lymphoma (HL) and systemic anaplastic large cell lymphoma (sALCL), there is a need for alternative approaches to maximise control of the lymphoma in refractory and relapsed cases. Antibody–drug conjugates (ADCs) allow specific targeting of drugs to neoplastic cells. The ADC brentuximab vedotin (BV) has the ability to target cluster of differentiation (CD) 30+ tumour cells and initiate cytotoxic effects. In two phase II trials, BV resulted in objective responses in 75 % and 86 % of patients with refractory or relapsed HL and sALCL, respectively, with an acceptable toxicity profile. Based on these data, BV was granted accelerated approval by the US Food and Drug Administration for the treatment of refractory and relapsed HL and ALCL. A promising indication for BV is acting as a bridge to stem cell transplantation (SCT). Numerous studies are currently examining the role of BV as salvage therapy prior to autologous or allogeneic SCT, as well as in other clinical settings.

scholarly journals Advances in Acute Myeloid Leukemia: Recently Approved Therapies and Drugs in Development

Cancers ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 3225 ◽  
Author(s):  
Michele Stanchina ◽  
Deborah Soong ◽  
Binbin Zheng-Lin ◽  
Justin M. Watts ◽  
Justin Taylor
Keyword(s):  
Acute Myeloid Leukemia ◽  
Myeloid Leukemia ◽  
Checkpoint Inhibitors ◽  
New Drugs ◽  
Cell Transplant ◽  
Antibody Drug Conjugates ◽  
Molecular Abnormalities ◽  
Drug Conjugates ◽  
Acute Myeloid ◽  
Antibody Drug

Acute myeloid leukemia (AML) is a genetically heterogeneous malignancy comprised of various cytogenetic and molecular abnormalities that has notoriously been difficult to treat with an overall poor prognosis. For decades, treatment options were limited to either intensive chemotherapy with anthracycline and cytarabine-based regimens (7 + 3) or lower intensity regimens including hypomethylating agents or low dose cytarabine, followed by either allogeneic stem cell transplant or consolidation chemotherapy. Fortunately, with the influx of rapidly evolving molecular technologies and new genetic understanding, the treatment landscape for AML has dramatically changed. Advances in the formulation and delivery of 7 + 3 with liposomal cytarabine and daunorubicin (Vyxeos) have improved overall survival in secondary AML. Increased understanding of the genetic underpinnings of AML has led to targeting actionable mutations such as FLT3, IDH1/2 and TP53, and BCL2 or hedgehog pathways in more frail populations. Antibody drug conjugates have resurfaced in the AML landscape and there have been numerous advances utilizing immunotherapies including immune checkpoint inhibitors, antibody-drug conjugates, bispecific T cell engager antibodies, chimeric antigen receptor (CAR)-T therapy and the development of AML vaccines. While there are dozens of ongoing studies and new drugs in the pipeline, this paper serves as a review of the advances achieved in the treatment of AML in the last several years and the most promising future avenues of advancement

scholarly journals An overview of antibody–drug conjugates in oncological practice

2020 ◽  
Vol 12 ◽  
pp. 175883592096299
Author(s):  
Charalampos Theocharopoulos ◽  
Panagiotis-Petros Lialios ◽  
Helen Gogas ◽  
Dimitrios C. Ziogas
Keyword(s):  
First Generation ◽  
Cancer Therapeutics ◽  
Therapeutic Index ◽  
General Tendency ◽  
Antibody Drug Conjugates ◽  
Therapeutic Modalities ◽  
Drug Conjugates ◽  
The Us ◽  
Oncological Practice ◽  
Antibody Drug

Antibody–drug conjugates (ADCs) are designed to manipulate the toxic efficacy of specific chemotherapeutic compounds, employing the high affinity of antibody-mediated delivery so as to drive them selectively to target cancer cells. These immunoconjugates encompass the general tendency towards precision medicine and avert the systemic toxicities of conventional chemotherapy, accomplishing an improved therapeutic index. Cumulative experience acquired from first-generation ADCs offers new perspectives to these promising therapeutic modalities for various hematological and solid cancers and propels their clinical development in a faster-than-ever pace, as indicated by the approval of four novel ADCs during the last year. This paper aims to provide an up-to-date overview of the eight ADCs approved by the US Food and Drug Administration and their current indications in oncological practice. Starting from their bio-pharmaceutical background, we track their clinical evolution, with an emphasis on the pivotal trials that led to their commercial release. Late-stage studies examining these eight ADCs in other-than-approved settings as well as the investigation of potential new candidates are also reviewed. In the close future, more data are expected to expand ADCs’ oncological utility and to further reshape their role in cancer therapeutics.

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