indications

VX-150 is a highly selective NaV1.8 inhibitor relative to the other sodium channel subtypes (>400-fold).

Acebutolol hydrochloride (Acebutolol HCl) acts as a cardioselective beta-adrenergic antagonist with little effect on bronchial receptors and has intrinsic sympathomimetic properties. Acebutolol hydrochloride is the hydrochloride salt form of acebutolol, a synthetic butyranilide derivative with hypotensive and antiarrhythmic activity. Having stabilizing and quinidine-like effects on cardiac rhythm, Acebutolol hydrochloride is used in ventricular arrhythmias. Other indications include hypertension, alone or in combinations with other agents.

Trans-Tranilast is an antiallergic drug developed by Kissei Pharmaceuticals. It was approved in 1982 for use in Japan and South Korea for bronchial asthma. Indications for keloid and hypertrophic scar were added in 1993. It has been used for the treatment of allergic disorders such as asthma, allergic rhinitis and atopic dermatitis.

Acetazolamide sodium (OT-302 sodium) is a potent carbonic anhydrase (CA)IX inhibitor with diuretic, antigonococcal, and antihypertensive activity and may be used for indications such as epilepsy, glaucoma, edema, and altitude sickness.

AVX 13616, Avexa's leading antibacterial candidate, demonstrates significant in vivo antibacterial efficacy, especially against drug-resistant Staphylococcus pathogens, with an IC50 value of 2-4 µg/ml (MICs) and is targeted as an antibacterial agent. Comparable in activity to mupirocin within a nasal decolonization model, AVX13616 necessitated only a single application for effectiveness. This compound, alongside others, exhibited broad-spectrum antibacterial action, achieving MICs of 2-4 micrograms per milliliter against various isolates, including S. aureus, coagulase-negative staphylococci, enterococci, MRSA, VISA, and VRSA. Aimed for topical use and the treatment of wound infection or catheter-related infections, a solitary 5% (w/w) AVX13616 application (roughly equivalent to 2% mupirocin) proved as efficacious as twice-daily 2% mupirocin over five days in decolonizing MRSA in mice.

Biperiden Hydrochloride (KL 373 Hydrochloride) is an antiparkinsonian agent, which is the selective central M1 cholinoreceptors blocker and it is used for the adjunctive treatment of all forms of Parkinson's disease (postencephalitic, idiopathic, and arte

PB94 is a selective inhibitor of HDAC11 with an IC50 value of 108 nM. This compound can be radiolabeled as [11C]-PB94 for use in positron emission tomography (PET) to study brain uptake and metabolic characteristics in living animals. Furthermore, PB94 has been shown to alleviate neuropathic pain in mice and is applicable for research into neurological indications.

D-4418 is a PDE4 inhibitor. It has been in development as a novel anti-inflammatory therapy with asthma and chronic obstructive pulmonary disease being primary indications.

IACS-010759 hydrochloride is an orally potent and selective OXPHOS inhibitor that inhibits proliferation and induces apoptosis in OXPHOS-dependent brain cancer and acute myeloid leukaemia models for the study of relapsed/refractory AML and advanced solid tumours.

Hexanoyl glycine is an acylated amino acid that is used as a urinary biomarker for several indications. It is normally biosynthesized from hexanoyl-CoA and glycine by the mitochondrial enzyme glycine N-acyltransferase. Increased urinary excretion of hexanoyl glycine in humans is indicative of a deficiency in medium-chain acyl-CoA dehydrogenase. Increased urinary hexanoyl glycine can also be used as a biomarker for exposure to gamma radiation. Levels of hexanyl glycine can also be elevated during cancer, while they are decreased 20-fold in mice following treatment with the PPARα ligand Wy 14643.

CLP290 is an activator of the neuron-specific K+-Cl cotransporter KCC2 and displays potential for the treatment of a wide range of neurological and psychiatric indications.

Ar-V7-IN-1 (compound 47) is a potent inhibitor of Ar-V7, a genetic mRNA splice variant of the androgen receptor (AR) associated with resistance to AR-targeted therapy in patients with desmoplasia-resistant prostate cancer (mCRPC).

PF-376304 is a nonspecific PI3K inhibitor under development for anti-inflammatory indications. Phosphoinositide 3-kinase (PI3K) is an enzyme fundamental to the regulation of various metabolic processes.

PF-303 is a covalent-reversible BTK inhibitor. Inhibitors of Bruton's tyrosine kinase (BTK) possess much promise for the treatment of oncologic and autoimmune indications.

GB1874 is an inhibitor of the Wnt pathway targeting β-catenin-TCF4 protein-protein interaction (PPI), affecting proliferation and stemness in Wnt-dependent colorectal cancer (CRC) cells and inhibiting the growth of HCT116 tumour xenografts in vivo.

Nisevokitug (NIS-793) is a humanized IgG2λ monoclonal antibody that specifically neutralizes transforming growth factor-beta (TGF-β, isoforms TGFB1/TGFB2) and is expressed in CHO-K1 cells. this agent is currently being studied preclinically and clinically for its significant ability to modulate the immunosuppressive tumor microenvironment in various oncological indications.

Eclutatug (ALE C04) is a humanised antibody targeting claudin-1 (CLDN1), which can be used for the treatment of tumours and organ fibrosis indications, such as head and neck squamous cell carcinoma (HNSCC).