Baxdrostat
Roche, CinCor and AstraZeneca announced that baxdrostat (Baxfendy®), the first oral selective aldosterone synthase inhibitor, received FDA approval in May 2026 for hypertension. The drug shows more than 100‑fold selectivity for CYP11B2 versus CYP11B1, overcoming a long‑standing specificity hurdle. In the Phase 3 BaxHTN trial, daily 1 mg and 2 mg doses produced clinically significant blood‑pressure reductions, meeting primary and secondary endpoints. Baxdrostat is also advancing in Phase 3 studies for chronic kidney disease and heart failure.
Locking the Sec61 Gate to Corral Disease
Researchers are developing small‑molecule inhibitors that lock the Sec61 translocon in its closed conformation, preventing pathogenic proteins from entering the endoplasmic reticulum. Pre‑clinical studies show that these blockers can suppress the secretion of pro‑inflammatory cytokines and reduce tumor growth in...
Linerixibat
Linerixibat (brand name Lynavoy®), an oral ASBT/IBAT inhibitor, received FDA approval in March 2026 for treating cholestatic pruritus in patients with primary biliary cholangitis (PBC). The drug works by blocking ileal bile‑acid reuptake, addressing the bile‑acid dysregulation that drives severe itching....
NVP-INE963
Novartis and Medicines for Malaria Venture have advanced NVP‑INE963, an oral fast‑acting blood‑stage antimalarial, into Phase 2 trials. The candidate emerged from a 1.5 million‑compound phenotypic screen and shows activity against multidrug‑resistant Plasmodium falciparum, though its mechanism remains unknown. Preliminary Phase 2 data...
Sonrotoclax (BGB-11417)
Sonrotoclax (Beqalzi®) received FDA approval in May 2026 for patients with relapsed or refractory mantle‑cell lymphoma who have failed at least two prior therapies. The drug is an oral Bcl‑2 inhibitor engineered from the venetoclax scaffold to improve potency against both...
Module 4 Quiz
Drug Hunter has released a Module 4 quiz covering its Protein Structure & Target Pharmacology course. The assessment tests learners on every section of the module, reinforcing concepts essential for drug discovery. Access to the quiz requires a paid subscription, which...
Tazemetostat
Tazemetostat (Tazverik®) is the first oral EZH2 inhibitor approved by the FDA, initially for epithelioid sarcoma and later for follicular lymphoma with stronger activity in EZH2‑mutant patients. The sarcoma indication showed a modest 15% overall response rate, while the lymphoma...
Acoziborole
Acoziborole is a single‑dose oral drug that targets the CPSF3 enzyme to treat human African trypanosomiasis, commonly called sleeping sickness. Developed through a partnership between DNDi, Sanofi, Scynexis, and Anacor, the compound belongs to the novel benzoxaborole class. In a...
Milsaperidone
Milsaperidone (Bysanti®) received FDA approval in February 2026 for adult schizophrenia and for acute manic or mixed episodes of bipolar I disorder. The drug is a triple antagonist of D2R, 5‑HT2AR and α1AR and is a metabolite of the earlier antipsychotic iloperidone....
PF-06826647
Ropsacitinib (PF‑06826647) is an oral TYK2 kinase‑domain inhibitor that progressed to Phase 2b trials for plaque psoriasis and hidradenitis suppurativa. Unlike the approved TYK2 drug deucravacitinib, which binds the JH2 pseudokinase domain, ropsacitinib engages the active JH1 kinase domain, offering a...
Paclitaxel
Paclitaxel (Taxol®) received its first FDA approval in 1992 for ovarian cancer and has since become a cornerstone therapy for breast, lung and other solid tumors. The drug is a natural product isolated from the bark of the Pacific yew...
Degrader–Antibody Conjugates: Can Targeted Delivery Improve Tolerability?
Degrader‑antibody conjugates (DACs) fuse small‑molecule protein degraders to targeting antibodies, aiming to deliver the degrader selectively to disease‑relevant cells. Early pre‑clinical studies show that DACs can achieve potent target knock‑down while sparing healthy tissue, translating into a markedly better safety...
Module 4, Section 3: Selectivity and Site
The fourth lecture in the Protein Structure & Target Pharmacology module examines how drug discovery teams achieve selectivity. It outlines strategies for designing ligands that discriminate across the entire proteome, within closely related protein families, and even between proteins that...
TRI-611
TRI‑611 is a CNS‑penetrant, CRBN‑mediated molecular‑glue degrader targeting ALK fusion proteins in ALK‑positive non‑small cell lung cancer (NSCLC). By recruiting a non‑G‑loop degron distal to the orthosteric site, it degrades ALK independently of the active site, sidestepping common tyrosine‑kinase inhibitor...
AMX-883
Amphista Therapeutics announced AMX-883, an oral degrader that recruits the DCAF16 E3 ligase to eliminate the epigenetic reader BRD9. The preclinical program demonstrates selective BRD9 degradation in acute myeloid leukemia (AML) cell models, leveraging a previously identified BRD9 binder for...