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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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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Metabolite Tales Blog

APRIL 10, 2024

Where data was publicly available, the routes of human metabolism for each of the drugs in this subset is listed in Table 1. Metabolites found in humans are also observed in monkeys, and all metabolites were found to possess <10% of the activity of the parent drug. of the administered radiolabel in the human ADME study.

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Sygnature Discovery

NOVEMBER 29, 2023

Patients at a clinical cancer center in Michigan, USA, have been dosed with the experimental drug QN-302, a potential first-in-class novel treatment for advanced or metastatic solid tumors. In January 2023, QN-302 received Orphan Drug Designation by the FDA for the potential treatment of pancreatic cancer.

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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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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 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

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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The Pharma Data

JULY 2, 2023

Marcus Conrad from Helmholtz Munich discovered a novel anti-cancer drug, called icFSP1, which sensitizes cancer cells to ferroptosis. Although FSP1 has been considered as an attractive drug target for cancer therapy, in vivo efficacious FSP1 inhibitors have been lacking.

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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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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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Sygnature Discovery

NOVEMBER 29, 2023

Patients at a clinical cancer center in Michigan, USA, have been dosed with the experimental drug QN-302, a potential first-in-class novel treatment for advanced or metastatic solid tumors. In January 2023, QN-302 received Orphan Drug Designation by the FDA for the potential treatment of pancreatic cancer.

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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

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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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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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.

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The Pharma Data

FEBRUARY 25, 2022

Food and Drug Administration (FDA) has accepted for review the Prior Approval Supplement (PAS) to the Biologics License Application (BLA) for ABRILADA™ (adalimumab-afzb) as an interchangeable biosimilar to Humira® (adalimumab). Pfizer Inc. NYSE: PFE) today announced that the U.S.

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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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The Pharma Data

NOVEMBER 11, 2020

CREATES CENTRE OF EXCELLENCE FOR STRUCTURE-BASED DRUG DESIGN. INCREASES GLOBAL CAPACITY FOR HIGH-VALUE INTEGRATED DRUG DISCOVERY AND COMMERCIAL DEVELOPMENT OFFERING. CREATES UNIQUE CO-LOCATED, FULLY-INTEGRATED, HIGH-CAPACITY R&D CENTRE.

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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

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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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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Drug Target Review

OCTOBER 4, 2023

Antibody-drug conjugates (ADCs) have been a groundbreaking approach to cancer treatment with their ability to deliver cytotoxic drugs directly to diseased cells while sparing healthy tissues. 1 However, efforts proved less effective than the original drugs, owing mostly to insufficient toxicity against cancer cells.

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The Pharma Data

AUGUST 29, 2020

FDA and EMA have granted orphan drug designations to LNP023 for PNH and the rare renal disease complement 3 glomerulopathy (C3G). The FDA and EMA have granted orphan drug designations to LNP023 for the treatment of PNH and C3G. Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.

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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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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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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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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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The Pharma Data

NOVEMBER 4, 2020

Food and Drug Administration (FDA) Breakthrough Therapy and Fast Track Designations, is now in pivotal testing, and CTP-692 for schizophrenia is currently on track for topline data readout in the first quarter of 2021,” said Roger Tung, Ph.D., CTP-543 for moderate to severe alopecia areata, which received U.S.

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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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New Drug Approvals

SEPTEMBER 29, 2024

link] 01 Aug 2022 Cortexyme is now called Quince Therapeutics You need to be a logged in or subscribed to view this content This small molecule is an orally available protease inhibitor targeting the lysine proteases of the periodontal pathogen Porphyromonas gingivalis. All were deemed unrelated to drug. J Alzheimers Dis Rep.

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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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Agency IQ

JUNE 9, 2023

FDA finalizes new guidance on nonclinical assessment of potential immunotoxicity Late last week the FDA released a final guidance document containing recommendations on the nonclinical assessment of potential immunotoxicity for drugs and certain biologics.

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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

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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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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