Chemenu

Casdatifan (AB521) is a small molecule inhibitor of the oxygen-sensing transcription factor HIF-2⍺ that has demonstrated potent antitumor activity in xenograft models of renal cell cancer (RCC). Under normal physiological conditions, HIF-2⍺ is involved in sensing oxygen availability in multiple organs. In certain tumors, particularly clear cell RCC (ccRCC), HIF-2⍺ activity is highly dysregulated as a result of genetic abnormalities in the VHL pathway. This creates a situation of pseudohypoxia and the abnormal increase in HIF-2⍺-mediated expression of a wide array of proteins involved in cancer cell proliferation and survival, treatment resistance and angiogenesis. Chemenu has been working to develop more compounds for drug discovery. Here come the building blocks we can provide: https://lnkd.in/gnuxwFzT

XRad Therapeutics announced that the first patient has been dosed in the company’s Phase 1a trial evaluating XRD-0394 in combination with radiation therapy for the treatment of metastatic, locally-advanced or recurrent solid tumors. XRD-0394, is a first-in-class dual inhibitor of ataxia-telangiectasia mutated (ATM) and DNA-dependent protein kinase (DNA-PK). Initial development efforts are focused on evaluating XRD-0394’s ability to enhance radiation therapy when used in combination. In parallel, the company is exploring the potential benefits of using XRad’s dual kinase inhibitors in combination with targeted radionuclides, immune checkpoint inhibitors, polyadenosine diphosphate-ribose polymerase inhibitors and antibody drug conjugates. Chemenu has been working to develop more compounds for drug discovery. Here comes the building blocks we can provide: https://lnkd.in/gypbaKwx Keywords: XRD-0394; ATM; DNA-PK; cancer; building blocks  

Nested Therapeutics’ lead program, NST-628, is an oral, brain-penetrant pan-RAF-MEK non-degrading molecular glue that lacks paradoxical pathway activation through the prevention of RAF paralog heterodimerization. By inhibiting the phosphorylation and activation of MEK by RAF, NST-628 targets a critical step in the RAS/RAF/MAPK signaling pathway. Preclinically, NST-628 results in broad efficacy, high tolerability, CNS activity across various RAS- and RAF-driven tumor models, and has the potential to deliver transformative clinical benefits both as a monotherapy and as a key component in combination therapies. Now, NST-628 has advanced to a Ph. I trial in patients with refractory MAPK pathway mutated/dependent advanced solid tumors. Chemenu has been working to develop more compounds for drug discovery. Here come the building blocks we can provide: https://lnkd.in/gZiEtnBV # NST-628 # Molecular Glue # RAF # MEK # RAS # MAPK # Chemenu # Building Blocks

Dementia with Lewy Bodies (DLB) is a rapidly progressive neurodegenerative disorder with a significant aging population and unmet health need. Alterations in p38 mitogen-activated protein kinases (MAPKs) are found to contribute to the neurodegenerative process in Alzheimer's disease (AD) and related dementias. CervoMed’s Neflamapimod (VX-745) is an oral, brain penetrant, small molecule inhibitor of the protein kinase p38α. It is designed to specifically target the mechanisms that cause dysfunction and degeneration of neurons in the basal forebrain cholinergic system. Neflamapimod has the potential of reversing synaptic dysfunction in the basal forebrain. The positive phase 2a data was published in Nature Communications, Neurology, and JPAD. Neflamapimod was granted Fast Track Designation by the FDA for DLB, and phase 2b enrollment was completed in June, 2024. Chemenu supports your scientific research and drug discovery. Check our product catalog: https://lnkd.in/gVHvZwqY #DLB #MAPK #p38 # inhibitor #Dementia #Neuro #smallmolecule #buildingblock

Pathalys pharma secures $105 million series B financing. Oversubscribed financing paves path to NDA submission and pre-commercialization efforts for upacicalcet.  Upacicalcet is a novel calcimimetic that can be delivered intravenously at the end of the hemodialysis session via pre-filled syringe and has been demonstrated to effectively reduce levels of parathyroid hormone(PTH) and may have a better tolerability profile for patients. Upacicalcet can be used in secondary hyperparathyroidism (SHPT) to address an unmet need in the management of advanced chronic kidney disease (CKD). Chemenu has been working to develop more compounds for drug discovery. Here comes the building blocks we can provide: https://lnkd.in/gsg24G8S Keywords: Upacicalcet; CaSR; secondary hyperparathyroidism (SHPT); building blocks  

Obesity is linked to overactivity of the endocannabinoid system that regulates appetite, fat storage, and insulin resistance. Cannabinoid receptor type-1 (CB1) belongs to the G protein-coupled receptor (GPCR) superfamily, and are found in the brain and peripheral tissues. Pharmacological blockers of CB1 receptors have demonstrated effectiveness in suppressing appetite, inducing weight loss, enhancing energy expenditure and speeding up metabolism. Novo Nordisk’s Monlunabant is a novel peripherally-acting CB1 receptor blocker. This target limits brain penetration and minimizes psychiatric side-effects. Monlunabant is developed for the treatment of metabolic disorders. The phase 2 trials for diabetic kidney disease and obesity is expected in the second half of 2024. Chemenu supports your scientific research and drug discovery. Check our product catalog: https://lnkd.in/guYEg4At #CB1 #receptor #blocker #antagonist #peripheral #Cannabinoid #Obesity #Metabolic

CPHI MILAN

ORIC-944 is a potent and selective allosteric inhibitor of PRC2 developed by ORIC Pharmaceuticals. Initiated dosing of ORIC-944 in combination with NUBEQA® (darolutamide) and in combination with ERLEADA® (apalutamide) in the ongoing Phase 1b trial for prostate cancer in first half of 2024. Entered into clinical trial collaboration and supply agreements with Bayer and Johnson & Johnson to support the ongoing Phase 1b trial of ORIC-944 in combinations with AR inhibitors for the treatment of prostate cancer. Chemenu has been working to develop more compounds for drug discovery. Here come the building blocks we can provide: https://lnkd.in/gH5Fu4uc # ORIC-944 # PRC2 # Darolutamide # Apalutamide # AR # Prostate Cancer # Chemenu # Building Blocks

IDRx announces $120 million series B financing to advance potential best-in-class new treatment for gastrointestinal stromal tumor (GIST). IDRX-42 is a potent, oral, highly selective KIT inhibitor targeting all major categories of activating and resistance mutations in patients with KIT-mutant GIST (including variants in exons 9, 11, 13 and 17). IDRX-42 was granted Orphan Drug designation by the FDA for the treatment of GIST. IDRX-42 is currently being evaluated in StrateGIST 1, a first-in-human Phase 1/1b study. In preclinical studies, IDRX-42 demonstrated superior antitumor activity compared to imatinib, the current first-line of therapy, in GIST human xenograft models expressing mutations in KIT exons 9 and 11. In xenograft models expressing secondary resistance mutations in KIT exon 13 or 17, IDRX-42 treatment resulted in potent and dose-dependent antitumor activity superior to the second-line standard of care agent, sunitinib. Chemenu has been working to develop more compounds for drug discovery. Here comes the building blocks we can provide: https://lnkd.in/gPJh_hem Keywords: IDRX-42; M4205; KIT inhibitor; GIST; building blocks  

The S1P1 receptor, a protein that plays a pivotal role in regulating immune response, interacts with S1P, a plasma lipid mediator. Remarkably, S1P regulates an array of physiological phenomena such as angiogenesis, inflammation, immunity, cell motility, and neurotransmitter release. Enter Cenerimod, a novel, potent, and selective S1P1 receptor modulator featuring unique signaling properties, while notably negating broncho‐ and vasoconstrictor effects. Hence, Cenerimod stands as a promising candidate in the quest for improved S1P1 receptor modulators. Chemenu has been working to develop more compounds for drug discovery. Here comes the building blocks we can provide: https://lnkd.in/gV4xs6ty Keywords: Cenerimod; ACT-334441; S1P1 receptor; building blocks