Course: MSc in Pharmaceutical Science and Drug Delivery Systems


Drug Discovery Technology

Drug Name: Omalizumab

Xolair is an asthma drug, which is commercial name of the generic drug Omalizubam. It is a monoclonal anti-immunoglobulin E antibody commercially sold under the name Xolair. The drug has been widely accepted as a therapeutic pathway for Asthma for adults and the younger population over 6 years old (Ding et al., 2022). The drug was developed in the US through the team up of Novartis Pharmaceuticals Corporation and Genentech, and the drug was approved in 2003. The drug went through multiple phases of drug development, such as target identification & validation, lead generation, lead optimisation and other stages, until it finally received FDA approval for clinical use in 2003 (Henriksen et al., 2020). This study focuses on the drug discovery process of Xolair or Omalizumab in the preclinical phase, such as target identification, validation, lead identification and optimisation, along with evaluating the potential use of technologies in this phase, as well as the development of a workplace for the experts that can be involved in a drug development team.

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Table of Contents

  • Introduction
  • 1. Element
  • 1.1. Stages of the drug discovery process of Xolair
  • 1.2. Suitable technology for stages of drug discovery
  • 1.3. Workplan for the drug discovery process from initial concept to phase
  • 2. Reflective statement
  • 2.1. Strength and weakness
  • 2.2. An Action plan
  • Conclusion
  • Reference list

1. Element

1.1.Stages of the drug discovery process of Xolair

Target identification & validation
The efficiency of the drug that ensures safety and efficiency is evaluated in this phase to acknowledge the efficiency of the drug in working on the identified druggable genome (Finan et al., 2017). In the case of target identification, after identifying the mechanism of anti-IgE allergy suppression, the scientists have identified the domain 52 amino acid residues present in mIgE, which is the target root of IgE production (Sinica, 2022). The drug discovery process has been further instigated with the identification of this target site.

Initially, the drug was named CεmX, which has been identified as a highly effective target site for the therapeutic anti-IgE actions to prevent allergic reactions among patients (Rodak et al., 2021). Due to the explicit usability and functionality of Omalizumab, it has been helpful for the manufacturers to gain approval for the drug as it binds to IgE or human immunoglobulin E and prevents its binding to the high-affinity IgE receptors (Pelaia et al., 2018). This inhibits the allergic reaction's mediators and helps manage allergic conditions. The drug molecule has a monoclonal structure consisting of C6450H9916N1714O2023S38 (Drug Bank, 2022). The structure of the drug has been mainly compared to the four batches of Omalizumab produced by SSF were subjected to comprehensive structural characterisation utilising a variety of conventional protein and carbohydrate analytical techniques (EMEA, 2022). Tests showed that Omalizumab was the main ingredient, with minor molecular variations of Omalizumab occurring consistently from batch to batch and being properly characterised using a variety of physicochemical methods as well as being evaluated for potency. In validating the target site of Omalizumab, the drug has an effective mechanism of action that helps inhibit IgE's binding to the high-affinity IgE receptor, which is taken up by ACPs, when environmental allergens enter the body.

On the other hand, the IgE binding inhibition interrupts the allergic cascade and regulates the immune response (Reibman, 2017). With this mechanism, Omalizumab has been found to have the potential to manage the allergic conditions of adult patients and those over 6 years old. Even though the drug has multiple side effects, such as infection, chest tightness, breathing issues, bronchospasm, hypotension and more, these can be managed with standard dosage control (Drug Bank, 2022). Moreover, with the maintenance of standard dosage protocols and controlled administration of the drug, safety in outcome can be promoted (Fox and Rotolo, 2021). In the process of drug discovery, the features of the drug, which have served for the validation of its target site, is its intervention with Ig E producing pathway to induce immune response for preventing allergic reaction as allergy is majorly triggered by hypersensitivity in the immune system of individuals through intravenous (IV) dosage of the drug.

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Lead generation

The lead generation process is based on identifying the leading compound of a drug that fundamentally participates in the interaction of the drug and the target molecule (Chandrasekaran et al., 2021). Omalizumab is the only monoclonal antibody genre drug clinically used as an add-on treatment for treating severe asthma incidents in patients. The drug's unique mechanism is to produce a safe and effective clinical outcome in the case of asthma patients (Ferrer et al., 2018). Evaluating the structural basis of Omalizumab therapy, it has been found that the drug's molecular structure provides a mechanistic insight into the disruptive nature of IgE inhibitors for accelerating the dissociation between the antigen and high-affinity IgE receptor (Pennington et al., 2016). The IgE molecule has two binding sites, one of which is the Fc?RIα (high-affinity receptor) binding site, and another one is present at the C?2-C?3 interface in IgE. Among these two binding sites of IgE, the Fc?RIα is mainly blocked by Xolair. The NCSor non-crystallographic symmetrycopies are present along the length of the domain of the C?3 residues of the drug, which makes the domain the drug epitope or the lead molecule, and they share the majority of its interaction with the IgE (Kariyawasam and James, 2020).

The HT (High Throughput) screening of the drug interaction in a crystalline form has identified that the target molecule's mutant form can inhibit the drug's ability. At the same time, it has also indicated the participation of the heavy chain of the antigen to be the primary mechanism for the drug's interaction and inhibition of allergic reactions (Gasser et al., 2020). To be specific about the mechanism of action of Xolair, in its target binding sites, Xolair prevents IgE from binding to high-affinity IgE receptors (Fc?RIα), which is generally present on the surface of basophils and mast cells (Toubi and Vadasz, 2020). The degree of release of allergic reaction mediators is constrained by a decrease in surface-bound IgE on Fc RI-bearing cells.

Lead optimisation

This phase of lead optimisation during drug discovery is the process of designing the drug and its dosages for clinical use, followed by the identification of the lead compound. This phase is crucial in the identification of preclinical candidates and their accumulation in the drug discovery processes. Moreover, advanced biotechnological analysis techniques are also applied in this phase for optimisation of the leading compound in clinical usage. Currently, the drug is administered to patients in various dosages ranging from 75 mg to 600 mg, varying for the age and condition of the patients seeking help (Xolair, 2022). Even though the drug has been the only one in its specified mechanism of anti-IgE activities, it has also been associated with multiple toxicities, which require safe dosage monitoring.
To be specific about the lead optimisation process for deciding on the dosage of Omalizumab that can help active require free IgE reduction to promote patient health as well as avoid the side effects associated with the drug (Kroes et al., 2021). Based on the weight and the initiating IgE level of 150-375 mg, subcutaneous injections every 2 or 4 weeks are the most effective dosage of the drug that optimises the patient's condition to avoid the implications of allergy-induced Asthma among the patients (Saco et al., 2021). This particular dosage range has shown the best results in managing allergic Asthma by lowering the degree of exacerbation and treatment dependency of the patients. Additionally, this dosage also shows clinical efficacy in the case of promoting optimal lung function and avoiding conditions like bronchodilators.

Along with having the best results in terms of clinical efficacy, the dodge between 150 and 375 mg subcutaneous injection of Omalizumab shows safe outcomes. To be specific, multiple side effects are associated with the administration of Omalizumab, including hypotension, bronchospasm and more such adverse and mild side effects (Cáceres et al., 2019). The administration of drugs within an optimised dosage range allows clinicians to promote health by avoiding these side effects and promoting patient outcomes in terms of health outcomes. However, the biotechnological analysis of the drug has identified that patient safety ranges with the administration of the drug dosage (Lee et al., 2020). Even though the 150-375 mg subcutaneous injection dosage is efficient enough to promote safety, the research during the drug development phase has highlighted a comprehensive range of dosages that helps promote patient outcomes in terms of individualised outcomes (Kroes et al., 2021). Therefore, the lead optimisation phase of the drug has listed a range of dosages and makes clinicians responsible for administering patients with the most suitable dosage to promote safety and manage patient conditions.

Drug development milestones

In addition to the successful synthesis or production of the drug, the milestones of the drug development process can also be highlighted in the study. To be specific, the concept of anti-IgE (Xioliar) was invented in 1987 by Dr Chang after the discovery of IgE in 1967 (Sinica, 2022). To start with the basics of a drug development process, Xolair's synthesis procedure involves three stages.The invention of the drug marked the way for the development of the drug.It has been mainly produced in a cell culture of batch-fed suspension. The stages of the drug synthesis process are Seed train stage, inoculum train stage and production stage (EMEA, 2022). After production, omalizumab-containing culture fluid is removed from the cells by centrifugation and may be stored in the refrigerator before purification for a short period.Following these techniques, the drug, Omalizubam or Xolair, was discovered in 1991, and it was the first drug discovered in the category of anti-IgE medication(Guntern and Eggel, 2020). After going through different phases of drug development, Xolair was finally approved for commercial use in 2003. Being specific about the process for approval, along with in-lab processes, I also involved clinical phases. The clinical test was conducted using three different set of population aging from 12 to 72 years old and the procedure continued for 2 weeks. After a run-in time to ensure a stable conversion to a common ICS (fluticasone propionate for Study 3; beclomethasonedipropionate for Studies 1 and 2), participants in each study were randomly assigned to receive either Xolair or a placebo (Center for Drug Evaluation and Research, 2022). Finally, the results have shown successful outcomes in terms of patient's asthma outcomes. The efficacy of the drug has been the primary reason for it getting approval from the FDA for being used clinically. After that, many drugs with a similar mechanism of action was found. Nevertheless, Omalizumab or Xolair still holds the reputation of being first in the type.

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Key areas that have influenced the success of the drug

Multiple areas of the effectiveness of Omalizumab have contributed to its approval and success in clinical use for a wide range of patient populations, from 6 years old children to adult patients. Even though the drug, Omalizumab, has multiple toxic impacts in terms of its side effects and adverse outcomes for pregnant women, it has been approved by the FDA for clinical use. One of the main factors contributing to the approval and successful utilisation of the drug for clinically managing Asthma induced by allergy is associated with the comprehensive range of dosage options it provides.

Another crucial point that can be sighted as a factor influencing the success of the drug, Omalizumab, is that it has been a single drug in the monoclonal anti-immunoglobin E antibody genre that has been clinically used for a long time. Unique mechanisms of this drug have contributed to its efficiency in decreasing airway inflammation caused by allergic reactions by innovating high-affinity IgE receptor binding to the IgE antigen. In addition to managing the issue of allergy-induced Asthma clinically, the administration of drugs in a safe process can also promote the long function of the patient. All of the benefits mentioned above have influenced the Omalizumab drug to get clinical approval and be used safely.

1.2. Suitable technology for stages of drug discovery
The drug discovery and development process can be led by utilising multiple technologies in different stages. Especially in the current era of digitisation, digital technology promotes exclusive efficiency of the drug development process to add to the efficiency of the process and its outcomes. Even though the drug Omalizumab was developed about 20 years ago, in the current era, the following diction lists some suitable technologies that can be used in the drug discovery stages, as mentioned above.

Stage 1: Target identification and validation- CADD

The computational interface can be regarded as a potential technology-based resource that can be used by the drug development team while working on the discovery of a drug in terms of the potential target site and outcomes expected from a drug. In the case of Omalizumab, the identification of IgE antigen and the target site of the drug has contributed to the facilitation of the drug development process. In the current era, the use of computational technology can be helpful for the drug development team to identify ongoing research on a specific genre of the drug along with its target site (Medina-Franco, 2021). This specific technology can also economise and accelerate the drug discovery process. CADD, or computer-aided drug design, is a recent technology that helps in the molecular modelling of the drug, rational drug designing, applying computational chemistry and more (Gurung et al., 2021). Therefore, the application of CADD can be a rational choice for the drug development team to promote the efficiency of the drug discovery process.

Stage 2: Lead identification- High throughput mechanism using Artificial intelligence

Lead identification is a crucial stage of drug discovery as it helps the team associated with the drug discovery process to identify the drug's molecular mechanism and its interaction with the genomic target site. As previously mentioned, HT or high throughput screening is essential to the lead generation or lead identification process. Even though the screening technology is quite beneficial for the generation of leads through molecular analysis of the drug molecule, the application of artificial intelligence has gained comprehensive acceptance from drug developers across the globe (Pham et al., 2020). The application of artificial intelligence with high throughput screening techniques allows the automation of the process. Additionally, it allows the application of a deep learning framework in the lead identification process, which is more optimised and efficient than a single use of screening without AI (Pham et al., 2021). Therefore, AI must be incorporated into the lead identification process of drug discovery to promote the efficiency of the process.

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Stage 3: Lead optimisation

Lead identification is one of the major stages for optimising identified lead in the lead optimisation stage, which applies biotechnology in the process. Advanced biotechnology facilitates the molecular modelling of the drug molecule and identifies the drug's effective dosage (Byrne et al., 2021). Therefore, the drug discovery process must use advanced biotechnology to enhance process effectiveness, especially in the case of lead optimisation.

1.3. Workplan for the drug discovery process from initial concept to phase 1

The initial concept phase of drug development refers to the early discovery of a drug. Phase 1 involves the preclinical test of testing healthy volunteers during the administration of the drug. Between the early discovery and the phase 1 testing, there is another stage named preclinical research, which involves the collection of a wide array of information for further drug development (FDA, 2022). The drug development process is likely to involve multiple experts with scientific knowledge, including pharmaceutical scientists, medicinal chemists, biologists, pharmacologists, biotechnologists, microbiologists and more such professionals (Coussens et al., 2018). However, the plan for involving specific professionals is different for each stage. The drug development work plan for the involvement of experts should be as follows:

Discovery and development: This phase will likely involve multiple experts, such as medicinal chemists, biologists, pharmacologists, pharmaceutical scientists and more (Coussens et al., 2018). The collaboration and participation of different experts add different areas of knowledge and expertise to make drug discovery efficient enough to lead it toward further stages and eventual clinical approval.

Preclinical research: In the preclinical phase, the process involves multiple processes such as research and development of the drug, performing different assays to identify drug efficiency, finding dosage and more. Multiple experts are required to perform these processes, including a team of pharmacists working on research and development, microbiologists, pharmaceutical scientists, biotechnologists and more (Romasanta et al., 2020).

Clinical development (Phase 1): this stage involves healthy volunteers evaluating the efficiency of the drug and its impact on the health of a healthy person. Even though the members of the drug development team is more or less similar in the last two phases, this phase shows the involvement of new members, such as doctors and nurse, who participates in evaluating and monitoring patient outcome with their expertise in health and patient care (Kumaraiah et al., 2021). Additionally, pharmaceutical scientists and pharmacologists can also be a part of the team in this phase.

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2. Reflective statement

2.1. Strength and weakness

In terms of strength, the research has helped me widely to understand the drug development process and the drug, Omalizumab. Additionally, the role of IgE in triggering other allergies influences asthmatic reactions in patients. Moreover, my research has found a comprehensive number of articles on the drug and its application. These factors can be regarded as the core strengths of the research, along with its efficiency in helping me develop knowledge and skill about writing a scientific report.

On the contrary, information regarding the drug's development process is needed in the existing source. Even though there were some sources, they could not be used due to accessibility issues. This gap in the information has created multiple problems in writing the report. Even though I have tried to align the write-up, the write-up can be irrelevant in some cases due to the shortage of information. Therefore, the lack of information and involvement of irrelevant information in some cases is the weakness of the research.

2.2. An Action plan

Regarding the action plan regarding the study's weakness, the following actions will be taken to lead future research.
• The next time, I will first focus on accumulating information and evaluating tier availability and accessibility on the online sources before choosing a topic.
• I will work on my ability to write reports with relevance to the research topic.

Conclusively, drug development involves multiple crucial stages, from early conceptualisation to final approval for the drug. In the case of Omalizumab, the concept development was initiated in 1987, and the company received approval from the FDA in 2003. Since approval, the drug has been clinically used for the treatment of allergen-induced Asthma widely due to its unique mechanism for inhibiting IgE binding to the high-affinity IgE receptors. In the current context, the development of such a drug can be led with multiple advanced technologies, such as AI and computational technology, along with the expert team to ensure the successful development of a drug.


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