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]. Enzymes involved include CYP1A2, CYP2C8, CYP3A4, CYP4F2, and aldehyde oxidase (AOX).

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Drug Target Review

JUNE 16, 2025

Unlike traditional pharmacokinetic (PK) studies that rely on plasma measurements alone, MSI, when combined with traditional histology, enables spatial mapping of drug distribution, metabolism and target engagement. Toxicological investigations play a key role in assessing drug safety and, importantly, inform development decisions.

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Alta Sciences

JANUARY 31, 2024

Pharmacokinetics, Pharmacodynamics and Toxicokinetics Demystified pmjackson Wed, 01/31/2024 - 14:55 Understanding the effects of a drug, and how it interacts with the body, and vice versa, is critical to ensure it is safe for human use. This is where pharmacokinetic (PK), pharmacodynamic (PD) , and toxicokinetic (TK) analyses step in.

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New Drug Approvals

JULY 2, 2025

Orforglipron ( LY-3502970 ) is an oral, non-peptide, small-molecule GLP-1 receptor agonist developed as a weight loss drug by Eli Lilly and Company. [1] Orforglipron ( LY-3502970 ) is an oral, non-peptide, small-molecule GLP-1 receptor agonist developed as a weight loss drug by Eli Lilly and Company. [1]

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DrugBank

OCTOBER 17, 2024

Data science has emerged as an innovative tool in the biopharmaceutical industry, leveraging the power of machine learning and artificial intelligence to drive innovation and efficiency across the entire drug development lifecycle.

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Drug Hunter

MAY 18, 2023

Dian Su’s journey from chemistry and proteomics to the DMPK of drug conjugates Following a different path comes naturally to Dian Su, Senior Director of DMPK at Bicycle Therapeutics. In her small molecule DMPK research, proteomics also served to identify reactive metabolites (e.g., Proteomics!

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DrugBaron

FEBRUARY 7, 2022

Finding small molecule drugs is much harder than finding a needle in a haystack – discovering the right arrangement of atoms to bind precisely to a protein target to elicit a particular response is a problem of vast dimensionality. Yet the situation with small molecules is even worse.

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Drug Target Review

SEPTEMBER 25, 2024

While these approaches often produce encouraging initial results, the development of drug resistance remains a major obstacle for long-term patient survival. Classically, rational drug combinations are designed to target two nodes in the same oncogenic signalling pathway.

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The Pharma Data

JANUARY 19, 2021

Dr. Clark Cheng, Chief Medical Officer and Executive Director of Aptorum Group, commented, “The clearance of our CTA application for ALS-4 drug represents a significant milestone for the company and one of a number of targeted strategic goals for 2021. About ALS-4.

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Practical Cheminformatics

JANUARY 8, 2024

Picking up where we left off in Part I , this post covers several other ML in drug discovery topics that interested me in 2023. Most of the LLM activity in the drug discovery space in 2023 was reported as preprints from academic groups. Most of the drug discovery examples were underwhelming. Here’s the structure of Part II.

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The Pharma Data

DECEMBER 20, 2020

Pending Health Canada’s approval, the Phase 1 trial is designed to test the safety, tolerability and pharmacokinetics of ALS-4 in healthy volunteers. ALS-4 is a novel small molecule adopting an anti-virulence (non-antibiotic) approach to address the growing unmet medical needs of infections caused by Staphylococcus aureus.

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The Pharma Data

OCTOBER 15, 2020

Vertex Pharmaceuticals has decided to give up on its experimental VX-814, a small molecule drug for the rare genetic disease Alpha-1 antitrypsin deficiency (AATD), canning the drug’s development after seeing lackluster results from an early phase 2 trial.

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LifeSciVC

APRIL 24, 2024

Is a novel target at the inflection point where enough evidence is available to suggest it may prove to be a compelling drug? and whether a molecule’s pharmacology can help to mitigate safety risk. In order to start building a case for or against a target, I like to start with genetics – first human and then mouse. in liver, in CNS)?

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New Drug Approvals

JUNE 25, 2025

Several drugs in five major categories, each acting by different mechanisms, are available for treating hyperglycemia and subsequently, NIDDM (Moller, D. E., “New drug targets for Type 2 diabetes and the metabolic syndrome” Nature 414; 821 -827, (2001 )): (A) Insulin secretogogues, including sulphonyl-ureas (e.g.,

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The Premier Consulting Blog

MAY 31, 2023

As a cornerstone of the drug development process, nonclinical investigational new drug (IND)-enabling studies are essential for supporting first-in-human (FIH) dosing for novel therapeutics. Pharmacology A typical IND-enabling package includes information on the primary, secondary, and safety pharmacology of the drug.

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Drug Target Review

NOVEMBER 1, 2023

3 Another recent development is the implication of ATX in neurological diseases, 6,7 as ATX levels are related to metabolic disorders in Alzheimer disease, and thus might be an interesting biomarker and drug target for this devasting pathology. Rational Design of Autotaxin Inhibitors by Structural Evolution of Endogenous Modulators.

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New Drug Approvals

OCTOBER 12, 2024

ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated proagent of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. Clin Pharmacokinet. 2016 ; Abushakra et al., Hey JA, et al.

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The Pharma Data

NOVEMBER 17, 2020

The study demonstrated favorable proof-of-concept for LYT-100’s tolerability and pharmacokinetic (PK) profile, which will also enable twice-a-day (BID) dosing of LYT-100 in future studies. The therapeutic dose of pirfenidone approved by the US Food and Drug Administration (FDA) for the treatment of IPF is 801 mg three times a day.

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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.

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Drug Target Review

JUNE 12, 2023

This molecule shows immense potential as a pan-TEAD inhibitor, targeting advanced solid tumours. TEAD proteins are crucial for tumour progression and drug resistance, making them an attractive focus for therapeutic interventions. ISM6331 is a Pan-TEAD inhibitor with novel scaffold with good IP space, discovered by Chemistry42.

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The Premier Consulting Blog

AUGUST 8, 2024

On July 31, 2024, the US Food and Drug Administration (FDA) announced Fiscal Year 2025 (FY2025) Prescription Drug User Fee Amendments of 2022 (PDUFA VII) fee rates for the review of human drug and biological product applications along with prescription drug program fees.

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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. Since there was no change in drug substance, the sponsor was able to reference the DMF.

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The Pharma Data

NOVEMBER 11, 2020

Food and Drug Administration (FDA) clearance of an Investigational New Drug (IND) application for SLV213 for the treatment of COVID-19 and has dosed the first subjects in a Phase 1 clinical study. While SLV213 can be dosed orally or intravenously, Selva is first advancing it as an oral drug candidate for COVID-19. About SLV213.

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Metabolite Tales Blog

FEBRUARY 16, 2024

This results in cleavage of the drug to two metabolites, M1 and M9, with only M1 retaining the 14C label. of total drug related material in plasma. Biotransformation studies which reveal significant cleavage of a drug could thus trigger a route involving dual radiolabelling. Eur J Drug Metab Pharmacokinet 48 , 411–425 (2023).

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Drug Target Review

JULY 12, 2023

These assays provide insights into the molecular mechanisms of disease biology and drug response, enabling the characterisation of gene expression profiles and deviations in diseased cells. This platform can help identify and optimise pharmacologic properties of new drugs.

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New Drug Approvals

APRIL 18, 2025

2] [3] The US Food and Drug Administration (FDA) considers it to be a first-in-class medication. [4] 1] [2] Adverse effects The US Food and Drug Administration prescription label for crinecerfont has a warning for acute adrenal insufficiency or adrenal crisis. [2] Food and Drug Administration (FDA) (Press release). January 2025.

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The Premier Consulting Blog

JANUARY 31, 2023

Food and Drug Administration (FDA) adopted an addendum to the guidance titled “ S1B(R1) Testing for Carcinogenicity of Pharmaceuticals ,” which had previously been finalized by the International Council for Harmonization (ICH). Pharmacokinetic and systemic exposure data is also important to consider. On November 1, 2022, the U.S.

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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. Glucuronidation is the most common phase II reaction observed in the metabolism of drugs in humans. In fact, rodents lack a human UGT1A4 homologue gene [3].

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New Drug Approvals

SEPTEMBER 10, 2024

g/mol 1929519-13-0 NBI-1065846 or TAK-041 Phase 2 (S)-2-(4-oxobenzo[d][1,2,3]triazin-3(4H)-yl)-N-(1-(4-(trifluoromethoxy)phenyl)ethyl)acetamide Zelatriazin ( NBI-1065846 or TAK-041 ) is a small-molecule agonist of GPR139. Zelatriazin, C 18 H 15 F 3 N 4 O 3 , 392.3 49 (2): 121–132. doi : 10.1124/dmd.120.000246. 120.000246.

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Alta Sciences

APRIL 17, 2024

Five Promising Treatment Areas in Early-Phase Drug Development in 2024 aasimakopoulos Wed, 04/17/2024 - 15:52 Early-phase drug development is an ever-changing landscape, as emerging science leads to new promising areas of research for the treatment of human health issues.

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The Pharma Data

JANUARY 19, 2021

This small molecule therapy is presently in Phase 1 clinical trial for mild to moderate Alzheimer’s disease (AD), which is supported by a NIA R01 grant in healthy aged volunteers. CLARKSVILLE, Md., 20, 2021 (GLOBE NEWSWIRE) — Neuronascent Inc. , About Neuronascent, Inc.

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The Pharma Data

DECEMBER 15, 2020

Many drug makers are investing in new science and hope to develop new therapeutics that address autoimmune disease. Scientists will be testing a drug class targeting the C-reactive protein (CRP) marker of acute inflammation in the body. They’ll use software that searches available drugs, as well as drug-like compounds.

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Molecular Design

FEBRUARY 7, 2023

We commonly invoke the free drug hypothesis (FDH) in drug design which means that we assume that the free concentration at the site of action is the same as the free plasma concentration (the term ‘free drug theory’ is also commonly used although I prefer FDH).

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The Pharma Data

OCTOBER 27, 2020

The company plans to tackle the existing challenges of precision medicine with a three-prong approach – developing better medicines for known cancer-driving mutations, developing drugs for targets previously thought to be undruggable, and finding new, untapped targets that could lead to even better drugs. The company’s $27.4

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The Pharma Data

AUGUST 21, 2020

The short-term goal of CARE is to provide a quick emergency response to the pandemic by testing existing drugs that were designed to treat other diseases against COVID-19. Novartis has agreed to contribute a carefully curated library of about 1300 small molecules with antiviral activity to the CARE project.

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New Drug Approvals

SEPTEMBER 13, 2024

8] [9] [10] The drug has been found to dose-dependently block fentanyl -induced miosis at 25 mg and 60 mg in humans (with minimal to no blockade at doses of 4 to 10 mg), suggesting that the drug significantly occupies and antagonizes the MOR at a dose of at least 25 mg but not of 10 mg or less. [10] 2] Aticaprant is taken by mouth. [1]

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The Pharma Data

APRIL 11, 2023

A focus of the presentation will be on the target engagement results and pharmacokinetics from its ongoing monotherapy dose-escalation study to explore a potential optimal dose and schedule to effectively inhibit AhR.

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