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Metabolism of 2023 FDA Approved Small Molecules – PART 2

Metabolite Tales Blog

APRIL 10, 2024

Table 1: Small molecule drugs approved by the FDA in 2023 with reported involvement of phase II mechanisms In vitro : In vivo differences Incubation of the SGLT2 (sodium-glucose co-transporter-2) inhibitor bexagliflozin in human liver microsomes points to metabolism through both oxidation and glucuronidation to 6 main metabolites.

Small Molecule

Small Molecule FDA Approval FDA Pharmacokinetics

Metabolism of 2022 FDA approved small molecule drugs PART 2

Metabolite Tales Blog

APRIL 4, 2023

Metabolism of 2022 FDA approved small molecule drugs part 2 Mixing it Up By Julia Shanu-Wilson In Part 1 of this topic we looked at metabolism of the small molecule drugs approved by the FDA in 2022 that were mediated by CYP3A4. Dermavant’s tapinarof is one such friend. 8 This is not the only point of interest.

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Small Molecule FDA Approval FDA Drugs

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Metabolism of 2023 FDA Approved Small Molecules – PART 1

Metabolite Tales Blog

JANUARY 23, 2024

Metabolism of 2023 FDA Approved Small Molecules – PART 1 By Julia Shanu-Wilson 2023 was a fruitful year for drug approvals by the FDA, with a crop of 34 small molecules out of a total of 55 new drugs [1]. References [1] 2023 Novel Small Molecule FDA Drug Approvals. Health Sci Rep. 6(10):e1610.

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Small Molecule FDA Approval FDA Pharmacokinetics

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Understanding the Elements of a Typical IND-Enabling Package

The Premier Consulting Blog

MAY 31, 2023

While the type, number, and design of these studies vary based on product-specific characteristics, IND-enabling packages submitted to the FDA generally include key information about the pharmacology, pharmacokinetics, and toxicology of the product. All these studies need to be performed under GLP.

Packaging

Packaging Pharmacokinetics Small Molecule Clinical Trials

Deconstructing the Diligence Process: An Approach to Vetting New Product Theses

LifeSciVC

APRIL 24, 2024

and whether a molecule’s pharmacology can help to mitigate safety risk. Especially for oligo or small molecule discovery and development, it’s important to understand whether there are highly homologous sequences or proteins that may be impacted by a given therapeutic approach. based on “tool” molecule precedent.

Production

Production Small Molecule Regulations Trials

Optimized 505(b)(1) and 505(b)(2) Clinical Pharmacology Programs to Accelerate Drug Development

The Premier Consulting Blog

JULY 31, 2024

In this blog, we explain the role of clinical pharmacology in drug development and demonstrate how the right strategy can accelerate development under the US Food and Drug Administration (FDA) 505(b)(1) and 505(b)(2) New Drug Application (NDA) pathways. Author: Jayesh Patel , Principal Scientist, Pharmacokinetics

Clinical Pharmacology

Clinical Pharmacology Drug Development Pharmacokinetics Drugs

N-glucuronidation: the human element

Metabolite Tales Blog

DECEMBER 13, 2023

N -glucuronidation: the human element By Julia Shanu-Wilson In our last blog of the year, we look at why N -glucuronidation of drugs is important in human drug metabolism. Conjugation of small molecule drugs to glucuronic acid is catalysed by several UGTs to frequently form N – and O -glucuronides. J Pharm Biomed Anal.

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Small Molecule Metabolic Stability Treatment Drugs

Weight-of-Evidence Assessments: Unpacking New Guidance on Carcinogenicity Testing

The Premier Consulting Blog

JANUARY 31, 2023

This blog post will explain how the WoE approach is used in toxicology studies and how the S1B(R1) addendum could affect your nonclinical program. Pharmacokinetic and systemic exposure data is also important to consider. 1,2,3 Its appendix offers case studies on the application of WoE in determining the utility of 2-year rat studies.

Small Molecule

Small Molecule Pharmaceuticals FDA Production

AI in Drug Discovery - A Highly Opinionated Literature Review (Part II)

Practical Cheminformatics

JANUARY 8, 2024

Gotta be SAFE: A New Framework for Molecular Design [link] A blog post by Edward Williams from Terray Therapeutics introduced Contrastive Optimization for Accelerated Therapeutic Inference (COATI). This novel embedding considers both the topological and three-dimensional structure of molecules. In this paper, the authors then used 1.1

Drugs

Drugs Small Molecule Bioinformatics Packaging

Metabolism-Mediated Loss of Radiolabel

Metabolite Tales Blog

FEBRUARY 16, 2024

The paper, written by a consortium of scientists from several big pharma companies, points out that discussions around multi labelling are happening with more frequency due to the increase in larger molecular weight small molecules being developed. Eur J Drug Metab Pharmacokinet 48 , 411–425 (2023). Drug Metab.

Small Molecule

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Steep FY2025 PDUFA Fee Increase: Ways to Reduce the Full Fee Rate for Repurposed Drugs

The Premier Consulting Blog

AUGUST 8, 2024

For example, pharmacokinetic (PK) data from a comparative BA study and PK modeling approaches (e.g., Typically, new drug development under the 505(b)(2) pathway requires less capital and time and has a higher success rate versus the 505(b)(1) pathway, where the Sponsor develops safety and effectiveness information from scratch.

Drugs

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Navigating the 505(b)(2) Pathway: No Two Drugs Are Alike

The Premier Consulting Blog

SEPTEMBER 11, 2024

The 505(b)(2) new drug application (NDA) pathway offers a unique opportunity for small molecule developers to bring innovative products to market more efficiently by leveraging existing data they do not own or have right of reference to. Human factors. The new formulation resulted in a drug product that was very viscous.

Drugs

Drugs Clinical Pharmacology Packaging Small Molecule

Five Promising Treatment Areas in Early-Phase Drug Development in 2024

Alta Sciences

APRIL 17, 2024

In this blog article, we review some of these areas of investigation where Altasciences has robust expertise and solution offerings. Several small molecule GLP-1R agonists, such as oral orforglipron, are in late-stage clinical development.

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Codon Digest: Injected Gene Editors

Codon

APRIL 2, 2023

Read Safety and pharmacokinetics of escalating doses of neutralising monoclonal antibody CAP256V2LS administered with and without VRC07-523LS in HIV-negative women in South Africa (CAPRISA 012B): a phase 1, dose-escalation, randomised controlled trial. Read Small-molecule aptamer for regulating RNA functions in mammalian cells and animals.

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The FDA Modernization Act 2.0: The End of IND-Enabling Toxicology Studies?

The Premier Consulting Blog

APRIL 25, 2023

In this blog post, we examine several alternative approaches to animal testing and how the FDA handles the application of these methods in specific scenarios. In the US, new small molecule drugs are developed under the requirements of Sections 505(b)(1) and 505(b)(2) of the FFDCA.

FDA

FDA Animal Testing Pharmacokinetics Pharmaceuticals

Metabolism of 2024 FDA Approved Small Molecules – PART 1

Metabolite Tales Blog

JANUARY 22, 2025

Metabolism of 2024 FDA approved small molecules part 1 By Julia Shanu-Wilson Involvement of active metabolites The number of small molecules approved by the FDA in 2024 totaled 31 out of 50 NMEs with 56% (28) of these comprising small molecule therapies. Clin Pharmacokinet. 2015 May;54(5):457-71.

Small Molecule

Small Molecule FDA Approval FDA Pharmacokinetics

Major biotransformation routes of aficamten

Metabolite Tales Blog

NOVEMBER 13, 2024

Our paper pick this month and latest blog describes the routes of biotransformation of Cytokinetics’ aficamten, a drug mainly eliminated by metabolism [1,2]. References [1] Pharmacokinetics, disposition, and biotransformation of the cardiac myosin inhibitor aficamten in humans. Drug Metab Pharmacokinet. Pharmacol Res Perspect.

Pharmacokinetics

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Drug Discovery Digest

Metabolism of 2023 FDA Approved Small Molecules – PART 2

Metabolism of 2022 FDA approved small molecule drugs PART 2

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Metabolism of 2023 FDA Approved Small Molecules – PART 1

Webinars

Understanding the Elements of a Typical IND-Enabling Package

Deconstructing the Diligence Process: An Approach to Vetting New Product Theses

Optimized 505(b)(1) and 505(b)(2) Clinical Pharmacology Programs to Accelerate Drug Development

N-glucuronidation: the human element

Weight-of-Evidence Assessments: Unpacking New Guidance on Carcinogenicity Testing

AI in Drug Discovery - A Highly Opinionated Literature Review (Part II)

Metabolism-Mediated Loss of Radiolabel

Steep FY2025 PDUFA Fee Increase: Ways to Reduce the Full Fee Rate for Repurposed Drugs

Navigating the 505(b)(2) Pathway: No Two Drugs Are Alike

Five Promising Treatment Areas in Early-Phase Drug Development in 2024

Codon Digest: Injected Gene Editors

The FDA Modernization Act 2.0: The End of IND-Enabling Toxicology Studies?

Metabolism of 2024 FDA Approved Small Molecules – PART 1

Major biotransformation routes of aficamten

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