Chemical Biology and Drug Design

FEBRUARY 6, 2025

Analysis of prevalence of ring, nonring, sp 3 -, and sp 2 -hybridized oxygen in approved drugs. For the first time, analysis of distribution of different types of oxygen from center of mass of a molecule. In approved drugs, majority of oxygen atoms are present within 4 from the COM of the molecule.

FDA Approval 100

FDA Approval FDA Small Molecule Pharmacokinetics 100

Covalent Modifiers

JUNE 29, 2025

In this work, we observed that the tyrosinase variant from Bacillus megaterium, termed megaTYR, has an increased tolerance for small-molecule thiol substrates, which can inhibit the activity of other tyrosinases. This was demonstrated by the conjugation of targeting proteins to drugs, fluorescent probes, and therapeutic enzymes.

Small Molecule 130

Small Molecule Drugs 130

Covalent Modifiers

JUNE 12, 2025

The modular structure of STAT3 nominates several of its protein domains as possible drug targets, but their exploitation with potential small-molecule inhibitors has been unevenly distributed so far, with past efforts highly favoring the conserved SH2 domain.

Small Molecule 130

Small Molecule Clinical Trials DNA Trials 130

Chemical Biology and Drug Design

APRIL 4, 2025

At present, there are few studies on the drug resistance of mIDH1 inhibitors. It is found that a significant cause for drug resistance is that IDH1 has mutation at the second site. Isocitrate dehydrogenase (IDH) is a key metabolic enzyme that catalyzes the conversion of isocitrate to -ketoglutaric acid (-KG).

Small Molecule 100

Small Molecule Drugs DNA Treatment 100

Covalent Modifiers

MAY 18, 2025

However, the molecular basis for specific inhibition of USP30 by small molecules has remained elusive. Collectively, our work establishes a generalizable chimeric protein-engineering strategy to aid deubiquitinase crystallization and enables structure-based drug design with relevance to neurodegeneration.

Engineering 147

Engineering Regulations Small Molecule Clinical Trials 147

Drug Target Review

JUNE 6, 2025

As antibody-drug conjugates (ADCs) gain traction across oncology and begin to expand into other therapeutic areas, a persistent challenge remains: the design and optimisation of payloads. The ADC itself is not necessarily a large molecule – it’s a small molecule with aspects of a large molecule, and vice versa.

Small Molecule 52

Small Molecule Pharmacokinetics Packaging Drugs 52

Nvidia Developer: Drug Discovery

DECEMBER 3, 2024

Their specificity reduces the likelihood of off-target effects, making them safer and often more effective than small-molecule drugs for complex conditions. As a result… Source

Small Molecule 121

Small Molecule Disease Drugs Science 121

Chemical Biology and Drug Design

MAY 10, 2025

Although it is currently only used in veterinary therapy, carprofen proves to be a molecule with a versatile therapeutic potential for human pharmacotherapy. Moreover, the molecule is a target in the drug discovery process for the development of new bioactive compounds.

Small Molecule 100

Small Molecule Drug Development Science Therapies 100

Drug Target Review

JULY 3, 2025

Given macro healthcare influences (eg, economic uncertainty, environmental changes) and the numerous available treatments for major diseases, drug developers may need to reassess their therapeutic strategies. This has led drug developers to unintentionally limit their potential within chosen therapeutic spaces.

Drug Development 64

Drug Development Drugs Animal Testing Engineering 64

PPD

NOVEMBER 11, 2024

It is hard to ignore some of the most pressing, long-term trends driving the push to accelerate innovation and progress in drug development. As a result, biopharma and biotech companies working to bring their drug pipelines to the market require deep expertise from trusted partners to help deliver critical therapies for their patients.

Drug Development 97

Drug Development Clinical Trials Drugs Small Molecule 97

New Drug Approvals

JULY 5, 2025

It is a small molecule with a dual mechanism of action, acting as both a complete estrogen receptor antagonist and a selective estrogen receptor degrader (SERD). Oral Administration: Palazestrant is an orally available drug. PALAZESTRANT CAS 2092925-89-6 OP-1250, VU35KM56Q4 449.6 ribociclib).

Small Molecule 62

Small Molecule Clinical Trials Pharmacokinetics FDA 62

Drug Target Review

JUNE 16, 2025

G protein-coupled receptors (GPCRs) are a highly validated drug target family – accounting for 30-35 percent of all approved drugs. Despite this, the therapeutic potential of targeting most GPCRs remains untapped, as only 10 percent of GPCRs have been drugged.

Disease 59

Disease Therapies Small Molecule Immune Response 59

Drug Target Review

JULY 10, 2025

Absorption, distribution, metabolism, excretion and toxicity – collectively known as ADMET – are among the most critical and challenging hurdles in small molecule drug discovery. Data sharing without compromise Drug discovery has long been characterised by a strong culture of secrecy.

Metabolic Stability 72

Metabolic Stability Drugs Drug Development Small Molecule 72

Chemical Biology and Drug Design

JULY 1, 2025

ABSTRACT The interaction of small molecule drugs with human serum albumin (HSA) after entering the human blood circulation system profoundly affects their distribution and absorption in the body, and further influences the activity.

Small Molecule 100

Small Molecule Drugs Research 100

Drug Target Review

JUNE 11, 2025

Drug development is plagued by complex challenges, but multimodal AI is unlocking new opportunities. By integrating diverse data sources – from genomics to clinical insights – this approach is accelerating drug discovery, improving patient stratification and boosting success rates.

Drugs 64

Drugs Clinical Trials Drug Development Pharmaceuticals 64

Chemical Biology and Drug Design

JANUARY 27, 2025

ABSTRACT Docetaxel (DTX) is the preferred chemotherapeutic drug for prostate cancer (Pca), but the emergence of resistance has significantly reduced its efficacy. Polyphyllin VII (PPVII), a small molecule natural product derived from the traditional herb Paris polyphylla, has shown anticancer potential.

Small Molecule 100

Small Molecule Treatment Production Drugs 100

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.

Drugs 52

Drugs Organic Chemistry Laboratories Pharmaceuticals 52

Drug Target Review

APRIL 7, 2025

The challenge of GPCR drug discovery G protein-coupled receptors (GPCRs) are one of the most desirable and challenging target classes in drug discovery, as their mutation can lead to a wide range of diseases such as cancer, cardiovascular disorders and neurological conditions.

Fragment Screening 52

Fragment Screening Drugs Biophysical Assays Small Molecule 52

Drug Target Review

APRIL 7, 2025

In a recent survey conducted by ICON, Plc, biomarker selection was identified by 35 percent of respondents as a top challenge among drug developers for phase I trials, second only to navigating regulatory compliance (- 38 percent). To qualify as endpoints, biomarkers used in early phases must be relevant to later stages of drug development.

Clinical Development 69

Clinical Development Clinical Trials Clinical Pharmacology Trials 69

The Pharma Data

JUNE 25, 2025

These modalities offer a new layer of precision in targeting diseases that are difficult to address with conventional small molecules or biologics. The move also reinforces a broader trend within the pharmaceutical industry: the growing interest in RNA-based therapeutics , including oligonucleotides and microRNA modulators.

RNA 52

RNA Clinical Trials Disease Small Molecule 52

Drug Target Review

NOVEMBER 25, 2024

As the CEO of iOnctura, an innovative oncology biopharmaceutical company she co-founded in 2017, Catherine has played a key role in advancing the development of highly targeted small molecules aimed at revolutionising cancer treatment. I went on to complete my MBA and PhD at The Institute of Cancer Research (ICR) in drug development.

Treatment 52

Treatment Small Molecule Clinical Trials Trials 52

Alta Sciences

JULY 3, 2025

Altasciences At CPHI Americas 2025 pmjackson Thu, 07/03/2025 - 13:41 In the ever-changing drug development world, staying agile is essential to enabling more informed decisions, faster. It’s a challenge that affects a large percentage of new drug candidates—one we’re passionate about helping to solve.

Small Molecule 52

Small Molecule Drug Development Pharmaceuticals Science 52

BioPharma Drive: Drug Pricing

JULY 8, 2025

Unlike most approved drugs, which work by turning cell signaling up or down like a dimmer switch, this approach aims to rid cells of problem proteins entirely. Earlier this year, the field got its best look yet at how well one common type of these drugs performs. Several have drugs in or near clinical testing.

Targeted Protein Degradation 142

Targeted Protein Degradation Small Molecule Disease Therapies 142

Drug Target Review

JUNE 2, 2025

Bioconjugates are rapidly emerging as a key frontier in targeted therapies, particularly through Antibody-Drug Conjugates (ADCs) , which combine antibodies with cytotoxic drugs to deliver more precise and effective treatments. The addition of Drug Product assets for cytotoxic substances completes the fully integrated offering.

Small Molecule 52

Small Molecule Engineering Therapies Drugs 52

Drug Target Review

DECEMBER 4, 2024

G protein-coupled receptors (GPCRs) represent a cornerstone of modern drug discovery due to their crucial role in regulating human physiology and their involvement in numerous diseases. In the early days, each GPCR target required its own structure-modulating ConfoBody to be identified before starting any drug discovery.

Small Molecule 122

Small Molecule Pharmacokinetics Therapies Immune Response 122

The Pharma Data

JUNE 12, 2025

The presentations highlight the ongoing progress and growing promise of the company’s innovative therapeutic platform, featuring its investigational oral CELMoD™ (Cereblon E3 Ligase Modulating Drugs) agents mezigdomide, iberdomide, and golcadomide, alongside its first-in-class, oral BCL6 (B-Cell lymphoma 6) ligand-directed degrader (LDD) BMS-986458.

Targeted Protein Degradation 40

Targeted Protein Degradation Small Molecule Treatment Disease 40

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]

Small Molecule 57

Small Molecule Clinical Trials Trials Pharmacokinetics 57

LifeSciVC

JULY 8, 2025

By Jason Campagna, CMO of Q32, as part of the From The Trenches feature of LifeSciVC In a recent essay, I argued that biotech is entering its strategic infrastructure moment, a shift from molecule-centric innovation to a layered capability stack beneath the therapeutic. It was about special operations warfare.

Hospitals 54

Hospitals Small Molecule Science Nurses 54

The Pharma Data

JUNE 9, 2025

Pimicotinib: A Promising CSF-1R Inhibitor Pimicotinib is an investigational small molecule developed by Abbisko Therapeutics Co., In parallel, we are working to file a New Drug Application (NDA) to the U.S. Food and Drug Administration, with additional filings planned in other markets.”

Treatment 40

Treatment Therapies Small Molecule Marketing 40

The Pharma Data

JUNE 24, 2025

In just three years, nine promising research projects have received funding under the program, setting the stage for innovative breakthroughs in drug discovery. A recent example is Bayer’s global license agreement with Puhe BioPharma , focused on an oral, small molecule PRMT5 inhibitor designed to selectively target MTAP-deleted tumors.

Pharma R&D 40

Pharma R&D Pharmaceutical Companies Pharmaceuticals Science 40

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.,

Small Molecule 62

Small Molecule Treatment Regulations Drugs 62

New Drug Approvals

APRIL 2, 2025

1] [2] It is a non- opioid , small-molecule analgesic that works as a selective inhibitor of Na v 1.8 2] [6] Suzetrigine is the first medication to be approved by the US Food and Drug Administration (FDA) in this new class of pain management medicines. [2] Suzetrigine CAS 2649467-58-1 Weight Average: 473.4 ESI-MS m/z calc.475.0922,

FDA 62

FDA Therapies Trials Treatment 62

FDA Law Blog: Biosimilars

JULY 2, 2025

Our team assists clients with a wide variety of quality and manufacturing regulatory topics for drugs and biologics. Reviewing test protocols and reports for small molecule or biologic drug programs. Specifically, manufacturing/testing procedures and compliance with cGMPs.

Small Molecule 52

Small Molecule Compliance Engineering FDA 52

New Drug Approvals

JULY 10, 2025

1] The US Food and Drug Administration granted the application for sebetralstat orphan drug designation. [4] “Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema” Journal of Medicinal Chemistry.

FDA 57

FDA Treatment Small Molecule International 57

New Drug Approvals

MAY 26, 2025

S2CID 253257260. ^ “With the right partner, Pfizer gains fast-track tag for previously shelved NASH drug” Retrieved 20 November 2023. Ervogastat CAS 2186700-33-2 Non-alcoholic Steatohepatitis (NASH) with Liver Fibrosis (FAST TRACK – U.S.) 1] Its development was previously halted by the company but resumed in 2022. [2]

Small Molecule 62

Small Molecule Production Trials Drugs 62

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.

FDA 62

FDA FDA Approval Drugs Trials 62

New Drug Approvals

JULY 12, 2025

1] [2] [3] KIN-3248 is a small molecule that targets and inhibits oncogenic fibroblast growth factor receptors (FGFRs). “Activity of KIN-3248, a next-generation pan-FGFR inhibitor, against acquired FGFR-gatekeeper and molecular-brake drug resistance mutations” Journal of Clinical Oncology. February 2022).

Production 62

Production Small Molecule Pharmacokinetics Clinical Trials 62