Drug Target Review

MAY 31, 2024

Incredible advances in machine learning-driven tools allow us to predict the 3D structure of previously unsolved proteins, unlocking the power of structure-based drug design for drugging these targets, and most recently, the ability to predict protein assemblies, which contain both the protein and putative small molecule binders.

Organic Chemistry 45

Organic Chemistry Computational Chemistry Small Molecule Disease 45

Codon

MARCH 19, 2024

Both Yamanaka and Gurdon shared the 2012 Nobel Prize in Physiology or Medicine. But there’s a catch: unlike with the small molecule drugs we are used to, the side effects of reprogramming can be far worse than a headache or nausea. John Gurdon (left) and Shinya Yamanaka (right). Credit: PA Images / Alamy.

DNA 56

DNA Small Molecule Regulations Laboratories 56

Codon

JUNE 11, 2024

In 2012 , they found it in the form of DNA polymerase, an enzyme that replicates the genome prior to cell division. Small molecules can randomly transit through the pore and create disruptions, and the polymerase ratchet mechanism is imperfect, occasionally causing DNA to temporarily reverse direction through the pore.

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DNA Engineering RNA Small Molecule 79

NIH Director's Blog: Drug Development

APRIL 7, 2015

After a whirlwind tour of the cutting-edge robotics facility for high throughput screening of small molecules, she joined me and NCATS Director Dr. Chris Austin in announcing that, thanks to an innovative public-private partnership, an experimental drug originally developed to fight cancer is now showing promise against Alzheimer’s disease.

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Disease Drugs Clinical Trials Science 40

The Pharma Data

OCTOBER 28, 2020

Ridgeline Therapeutics is one such company, established in 2012 and spun out of technology invented by founder and CEO Stan Watowich at the University of Texas Medical Branch.

Science 40

Science Clinical Trials Small Molecule Marketing 40

New Drug Approvals

SEPTEMBER 13, 2024

“LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders” Neuropharmacology. Rankovic Z, Hargreaves R, Bingham M (2012). 27 (12): 2012–2020. PMID 34826432. February 2014). 77 : 131–144.

Treatment 62

Treatment Clinical Trials Pharmacokinetics Pharmaceuticals 62

Agency IQ

APRIL 19, 2024

Although therapeutics have contributed to improvements in survival, the five-year relative survival rate for patients with MM was just 57% between 2012 and 2018. Note: Both analyses focused only on studies of small molecules, antibodies and biologics; studies of CAR T therapies were not included.

FDA 40

FDA Disease Trials Clinical Trials 40

Drug Target Review

JANUARY 5, 2024

Å resolution) 6 is now being targeted for small molecule inhibitor discovery and development, by exploiting emergent computational tools to identify potential candidate compounds in silico and then test these predicted inhibitors in in vitro biochemical assays. 2012;Chapter 2:Unit2 8. Epub 2012/03/03.

Small Molecule 59

Small Molecule Drugs Biochemical Assays Regulations 59

The Pharma Data

DECEMBER 27, 2020

BRUKINSA (zanubrutinib) is a small molecule inhibitor of Bruton’s tyrosine kinase (BTK), discovered by BeiGene scientists, that is currently being evaluated globally in a broad pivotal clinical program as a monotherapy and in combination with other therapies to treat various B-cell malignancies. 2012 Aug 2;120(5):947-59.

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Production Therapies Treatment Drugs 52

The Pharma Data

AUGUST 3, 2021

HLE BiTE ® molecules AMG 199 and AMG 910, targeting mucin 17 (MUC17) and claudin 18.2 AMG 176, a small molecule inhibitor of myeloid cell leukemia 1 (MCL-1), continues to enroll patients with hematologic malignancies. Tax Court to contest notices of deficiencies received from the IRS during the quarter for 2010, 2011 and 2012.

Biosimilars 52

Biosimilars Production Treatment FDA 52

The Pharma Data

JULY 21, 2021

Abrocitinib is an oral small molecule that selectively inhibits Janus kinase (JAK) 1. XELJANZ has been studied in more than 50 clinical trials worldwide, including more than 20 trials in RA patients, and prescribed to over 300,000 adult patients (the majority of whom were RA patients) worldwide since 2012. About Abrocitinib.

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FDA Clinical Trials Treatment Therapies 52

Drug Target Review

JANUARY 16, 2025

Traditionally, drug discovery has focused on small-molecule therapeutics, typically with a molecular weight of less than 500 Daltons. 2 Typically, small-molecule drugs target active sites buried inside proteins. What are macrocycles and why are they interesting for drug discovery?

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Drug Development Small Molecule Drugs FDA Approval 52

Drug Target Review

NOVEMBER 1, 2024

Strategies for the synthesis and development of complex active pharmaceutical ingredients While the prevalence of biologics has grown within the pharmaceutical sector over recent decades, small molecules remain important and can offer significant advantages. 2012, 75, 311–335, [link] 3 Krzyzanowski A, Pahl A, Grigalunas M, Waldmann H.

Small Molecule 52

Small Molecule Production Pharmaceuticals Drug Development 52

Drug Hunter

APRIL 24, 2023

The new laws include Medicare negotiation and includes a provision that disproportionately affects small molecules which have triggered reactions throughout the industry from the extreme of “this is the end of small molecule drug discovery as we know it” to “this may not cause permanent damage.”

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Small Molecule Drugs Biosimilars Vaccine 130