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] 1] It was discovered by Chugai Pharmaceutical Co. then was licensed to Lilly in 2018. [1] percentage points from a starting level of 8%. [1] kg), on average after 40 weeks. [1]

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ASPET

SEPTEMBER 16, 2024

Here, we describe 8015-P2, a new small molecule mitofusin activator with ~10-fold greater potency and improved in vivo pharmacokinetics vs comparators, and demonstrate its rapid reversal of sensory and motor neuron dysfunction in an Mfn2 T105M knock-in mouse model of Charcot-Marie-Tooth disease type 2A.

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Drug Target Review

APRIL 7, 2025

Novel mechanisms of action associated with CGTs naturally create dosing effects that apply in very different ways than with traditional small molecule pharmacotherapies. Trial design and statistical methods are also key to determining the utility and validity of biomarkers.

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Drug Hunter

MAY 18, 2023

From a childhood in a small village in China’s northeast Shandong province to her work examining the drug metabolism and pharmacokinetics (DMPK) of antibody-drug conjugates (ADCs) and Bicycle toxin conjugates ® (BTCs), Dian has always looked to forge something new. It built my confidence to build something from scratch.” 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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The Pharma Data

JANUARY 19, 2021

The secondary objective is to assess the pharmacokinetic profile of SAD and MAD of ALS-4 administered orally to healthy subjects. The primary objective of the trial is to evaluate the safety and tolerability of SAD and MAD of ALS-4 administered orally to healthy subjects. About ALS-4.

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Drug Target Review

SEPTEMBER 25, 2024

Applying our technology has enabled us to develop a new small molecule, TT125-802, and to assign a new role to the epigenetic regulator CBP/p300 as a novel master regulator of non-oncogene resistance. This orally available small molecule binds to the bromodomain of CBP/p300 in a highly specific manner.

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DrugBank

OCTOBER 17, 2024

Data Science in Lead Optimization and Drug Design Data science accelerates the lead optimization and drug design process, transforming how molecules are engineered for therapeutic applications. Furthermore, data-driven approaches can optimize clinical trial design, leading to smaller sample sizes and reduced overall costs.

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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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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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Drug Target Review

NOVEMBER 1, 2023

2,8-10 However, the number of compounds with satisfying pharmacokinetic parameters (PKD) are limited, with most unable to cross the blood-brain barrier or go sufficiently deep into a malignant tumour. Structure–Activity Relationships of Small Molecule Autotaxin Inhibitors with a Discrete Binding Mode. J Med Chem. J Med Chem.

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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. Photo: Business Wire).

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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.

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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. For instance, Cheng et al.

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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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Disease Small Molecule Pharmacokinetics Licensing 52

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. in liver, in CNS)?

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New Drug Approvals

JUNE 25, 2025

2011, 2 , 828-839 DOI: 10.1039/C1MD00116G [link] [link] Glucokinase is a key regulator of glucose homeostasis and small molecule activators of this enzyme represent a promising opportunity for the treatment of Type 2 diabetes. clinical candidate currently in Phase 2 development.

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The Pharma Data

NOVEMBER 11, 2020

As an orally bioavailable small molecule with broad antiviral activity, SLV213 could be a valuable treatment to meet today’s urgent need to fight COVID-19 as well other life-threatening infectious diseases, such as Chagas disease, Ebola virus disease, and Nipah virus infection.”. About SLV213.

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Drug Target Review

JUNE 12, 2023

The current version of Chemistry42 uses over 40 generative models, including generative autoencoders and generative adversarial networks as well as both structure-based and ligand-based drug design to generate and optimise de novo small molecules.

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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.

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The Premier Consulting Blog

JULY 31, 2024

Regulatory Pathway 505(b)(2) versus 505(b)(1) In the US, novel new small molecule drug products, including some peptides, are regulated, and approved by the FDA under the Federal Food, Drug, and Cosmetic Act (the “Federal FD&C Act”) under two key regulatory pathways: Section 505(b)(1) and Section 505(b)(2) NDAs.

Clinical Pharmacology 52

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Practical Cheminformatics

JANUARY 8, 2024

A Tutorial on Encoding and Generating Small Molecules with COATI [link] COATI: multi-modal contrastive pre-training for representing and traversing chemical space [link] The team at AstraZeneca released version 4 of their software package REINVENT for generative design. Drug discovery is inherently an MPO problem.

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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.

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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 88 (8): 3872–3882. doi : 10.1111/bcp.15305. PMC 9544063.

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The Premier Consulting Blog

JANUARY 31, 2023

Of note, this guidance is specific to small molecule pharmaceuticals; similar guidance for biologics can be found in the ICH’s S6(R1) Preclinical Safety Evaluation for Biotechnology-Derived Pharmaceuticals. Pharmacokinetic and systemic exposure data is also important to consider.

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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 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.

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Metabolite Tales Blog

DECEMBER 13, 2023

Conjugation of small molecule drugs to glucuronic acid is catalysed by several UGTs to frequently form N – and O -glucuronides. As in this example, most N -glucuronides of small molecule drugs are innocuous and possess no pharmacological activity. J Pharm Biomed Anal. Sundararaghavan VL, Sindhwani P, Hinds TD Jr.

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The Pharma Data

OCTOBER 27, 2020

Primmune aims to advance the development of their novel orally-administered, small molecule toll-like receptor 7 agonists as therapeutic-adjuvants for acute viral diseases and cancer. The company’s $27.4

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Drug Target Review

JULY 12, 2023

Once a new drug target is identified, a proprietary deep learning artificial intelligence (AI) platform we call Fluency can rapidly identify small molecules that selectively bind to a target of interest.

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The Pharma Data

DECEMBER 15, 2020

Small Molecule Inhibitors. NMD670 is a first-in-class small molecule inhibitor of the muscle specific chloride ion channel, the ClC-1 ion channel. The secondary outcome involves pharmacokinetic endpoints. Oral, Small Molecules. The primary outcome includes safety and tolerability endpoints.

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Molecular Design

FEBRUARY 7, 2023

The FDH is covered in the S2010 (see Box 1 and 2) and B2013 articles and, given that the targets of small molecule drugs tend to be intracellular, I’ll direct you to the excellent Smith & Rowland perspective on intracellular and intraorgan concentrations of drugs.

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The Pharma Data

AUGUST 21, 2020

Novartis has agreed to contribute a carefully curated library of about 1300 small molecules with antiviral activity to the CARE project. We are also supporting the consortium’s preclinical safety and pharmacokinetics workstreams. These will be screened against SARS-CoV-2. And this is just one of our multistakeholder engagements.

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The Pharma Data

JANUARY 17, 2021

18, 2021 /PRNewswire/ — Genkyotex SA , a subsidiary of Calliditas Therapeutics AB (publ) (“Calliditas”) (Nasdaq OMX – CALTX; NASDAQ – CALT), today announced positive Phase 1 data demonstrating a favorable safety and pharmacokinetic profile of high-dose setanaxib, Genkyotex’s lead asset. STOCKHOLM , Jan.

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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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The Pharma Data

OCTOBER 18, 2020

Several clinical sites are screening patients for the Phase 1 a/b multicenter, open-label, dose escalation study of safety, pharmacodynamics, and pharmacokinetics of CG-806 in ascending cohorts (3+3 design) to determine the maximum tolerated dose or recommended dose in patients with relapsed or refractory AML.

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