Drug Hunter

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A single-dose cure has arrived for HAT (human African trypanosomiasis). A benzoxaborole, acoziborole is a reversibly-cov...
06/03/2026

A single-dose cure has arrived for HAT (human African trypanosomiasis). A benzoxaborole, acoziborole is a reversibly-covalent binder of CPSF3 in Trypanosoma parasites that leaves human CPSF3 untouched. The compound’s late-stage optimization helped tune compound CNS exposure, resulting in a PK profile that delivered a 100% cure rate in a CNS mouse infection model.

Acoziborole delivered a 95% cure rate in a Ph. 2/3 trial as an oral 960 mg single-dose, curing patients in both early- and late-stage disease–differentiating itself from the other completely oral sleeping sickness regimen, fexinidazole, which is ineffective in severe stage 2 infections.

Following fexinidazole’s 2018 approval, acoziborole is the second fully oral treatment for HAT and the first single-dose cure. The drug received a positive scientific opinion from the EMA in February 2026 and awaits formal registration in endemic countries.

Read more on Drug Hunter: https://drughunters.com/4vsGcrb

Milsaperidone (Bysanti®) was approved by the FDA in February 2026 for the treatment of schizophrenia in adults and for t...
06/02/2026

Milsaperidone (Bysanti®) was approved by the FDA in February 2026 for the treatment of schizophrenia in adults and for the acute treatment of manic or mixed episodes associated with bipolar I disorder in adults.

Closely related to iloperidone (Fanapt®), milsaperidone reached the market through an unusually abbreviated development path. Because iloperidone and milsaperidone rapidly interconvert in vivo, Vanda was able to support approval with a Ph. 1-centered bioequivalence package bridging back to iloperidone.

That meant head-to-head studies in healthy volunteers and in patients with schizophrenia or bipolar I disorder were enough to help bring milsaperidone from first-in-human testing in 2021 to FDA approval in 2026.

Vanda developed both compounds, making Bysanti a notable example of how metabolite pharmacology, regulatory strategy, and lifecycle management can converge in CNS drug development.

Read it on Drug Hunter: https://drughunters.com/3PBu2x5

Ropsacitinib (PF-06826647) is a TYK2 inhibitor that reached Ph. 2 development in plaque psoriasis and hidradenitis suppu...
06/01/2026

Ropsacitinib (PF-06826647) is a TYK2 inhibitor that reached Ph. 2 development in plaque psoriasis and hidradenitis suppurativa.

What made it especially interesting was its mechanism: unlike deucravacitinib (Sotyktu®), which binds the TYK2 JH2 pseudokinase domain allosterically, ropsacitinib targeted the catalytically active JH1 domain—an ambitious strategy given how conserved the JAK ATP-binding site is.

Despite encouraging psoriasis data, ropsacitinib does not appear to be in active development today, while Priovant’s dual JAK1/TYK2 inhibitor brepocitinib has become the clearer priority.

Read more on Drug Hunter: https://drughunters.com/4xk9PwP

June is Alzheimer’s & Brain Awareness Month – and the urgency around neurodegenerative diseases drug discovery has never...
06/01/2026

June is Alzheimer’s & Brain Awareness Month – and the urgency around neurodegenerative diseases drug discovery has never been clearer.

Two mechanistically distinct approaches are generating serious scientific momentum, and our team at Drug Hunter published in-depth analyses on both:

-TREM2 Agonists in Neurodegeneration: TREM2 signaling sits at the intersection of microglial activation, synaptic pruning, and amyloid clearance. Our analysis covers the therapeutic potential, translational data, key pharmacological challenges, and the emerging competitive landscape surrounding TREM2-targeted approaches across Alzheimer’s disease and related neurodegenerative disorders.

-RNA Splice Modulators in CNS: Small molecule splice modulators are moving beyond their rare disease origins. The development of orally bioavailable RNA-targeting small molecules offer an advantage over existing RNA-targeting modalities such as siRNA, antisense oligonucleotides, biologics, and gene therapy. Our analysis discusses how RNA splice modulation strategies are being applied to complex CNS indications.

Both analyses are available with complimentary access following a short platform demo. Reach out or click the link below to schedule.

https://drughunters.com/43GBr1i

The Drug Hunter team reviews thousands of IP disclosures each month to highlight the most impactful drug discovery paten...
05/30/2026

The Drug Hunter team reviews thousands of IP disclosures each month to highlight the most impactful drug discovery patents.

For April 2026, we analyzed and curated a searchable dataset of the most noteworthy disclosures, offering key data, molecular insights, and therapeutic relevance.

Highlighted disclosures:
-1cBio: ENPP1 inhibitors for hypophosphatasia
-Arrakis Therapeutics: heterobinfunctional degraders of RNA targeting CNOT9
-Kaken Pharmaceutical: Small molecule STAT6 inhibitors
-Atrogi: biased β2-adrenergic receptor agonists for obesity and metabolic disease
-Para: VPS4A inhibitors targeting an untapped synthetic lethality relationship

Read the full article on Drug Hunter: https://drughunters.com/4uDVlWt

A method that enables rapid access to glutarimides has been reported in a collaboration between the Baran Lab and BMS. G...
05/29/2026

A method that enables rapid access to glutarimides has been reported in a collaboration between the Baran Lab and BMS.

Glutarimides are a key motif in the TPD (targeted protein degradation) field, and an array of scaffolds beyond those based on substituted thalidomides have entered clinical trials. However, only limited reports of glutarimides bearing α-sp3 hybridized substituents have emerged.

In this Chemistry Brief, we highlight a useful extension of the nickel-catalyzed cross-coupling of hydrazides pioneered by the Baran lab and its application to scaffolds relevant to heterobifunctional and molecular glue degraders.

Read it on Drug Hunter: https://drughunters.com/4dCRovl

Amino acids are the fundamental building blocks of proteins. Their primary sequence and the chemical properties of their...
05/29/2026

Amino acids are the fundamental building blocks of proteins. Their primary sequence and the chemical properties of their side chains govern protein folding, enzyme catalysis, and molecular recognition.

Explore our amino acids cheat sheet, which highlights the structures and key properties of the 21 amino acids found in the human proteome as well as their relevance in protein structure.

We hope this cheat sheet serves as both a valuable resource and inspiration for drug hunters at all stages of their careers.

Explore the cheat sheet on Drug Hunter: https://drughunters.com/49Uxb1K

Paclitaxel (Taxol®) is a natural product drug first FDA approved in 1992 for ovarian cancer that later became a backbone...
05/28/2026

Paclitaxel (Taxol®) is a natural product drug first FDA approved in 1992 for ovarian cancer that later became a backbone therapy across multiple cancers.

Isolated from Pacific yew tree bark, paclitaxel’s anticancer activity stems from its stabilization of microtubules, which suppresses microtubule dynamics and disrupts mitosis—a novel mechanism of action at the time that renewed enthusiasm for its clinical development.

Although the program was threatened by low isolation yields and the ecological burden of harvesting Pacific yew bark, a semi-synthetic route from the more readily available natural product precursor 10-deacetylbaccatin III enabled large-scale production and helped bring paclitaxel to patients.

Read more on Drug Hunter: https://drughunters.com/3PqR5us

Discovery of Bexobrutideg, an Oral Targeted Degrader of BTK for the Treatment of B-cell MalignanciesThursday, July 2nd, ...
05/28/2026

Discovery of Bexobrutideg, an Oral Targeted Degrader of BTK for the Treatment of B-cell Malignancies
Thursday, July 2nd, 2026
8 AM PT | 11 AM ET | 5 PM CET

BTK inhibitors targeting the orthosteric site of the protein are widely used for the treatment of B-cell malignancies. Despite significant progress, the emergence of BTK inhibitor resistant mutations is a persistent therapeutic challenge. In addition, BTK promotes BCR signaling through non-enzymatic scaffolding functions. These challenges highlight the need for therapies with an alternative mechanism of action. Bexobrutideg is an orally administered heterobifunctional small molecule degrader that acts to selectively eliminate both wild-type and mutant BTK from cells via cereblon-mediated ubiquitination and proteasomal degradation.

In this Flash Talk, Barbara Czako, Executive Director of Medicinal Chemistry at Nurix Therapeutics will share the discovery story, preclinical characterization and Phase 1a/b safety and efficacy data for bexobrutideg.

Register now to learn more about the discovery and preclinical and clinical findings surrounding this BTK degrader: https://drughunters.com/4nTrNBL

Mitochondrial uncouplers increase energy expenditure by allowing protons to cross the inner mitochondrial membrane indep...
05/27/2026

Mitochondrial uncouplers increase energy expenditure by allowing protons to cross the inner mitochondrial membrane independently of ATP synthesis. By disconnecting mitochondrial metabolism from energy storage, these compounds increase fatty acid utilization and can reduce oxidative stress, creating therapeutic opportunities in obesity, metabolic disease, and inflammatory disorders. Unlike conventional weight-loss therapies, mitochondrial uncouplers do not directly suppress appetite and may better preserve lean mass. However, clinical development has historically been limited by narrow therapeutic windows and hyperthermia-associated toxicity.

Recent advances in tissue-targeted prodrugs, controlled-release formulations, and next-generation protonophore scaffolds have renewed interest in the field. In parallel, low-dose mitochondrial uncoupling has shown promising effects in preclinical models of neurodegenerative disease, suggesting potential applications beyond metabolic disorders.

After decades defined by on-mechanism toxicity, a new generation of mitochondrial uncouplers is now emerging with the potential to reshape how mitochondrial metabolism is therapeutically targeted.

Read more on Drug Hunter: https://drughunters.com/4nTFAbp

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