oral drug

ABBV-744 is a BDII-selective BET bromodomain inhibitor that inhibits BRD2 3 4. It is used in the research on inflammatory diseases, cancer, and AIDS.

Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.

Moxidectin (CL301423) is an anthelmintic drug which kills parasitic worms, and is used for the prevention and control of heartworm and intestinal worms. It can be found in treatments prescribed for animals such as dogs, cats, horses, cattle and sheep. Application methods for moxidectin vary by treatment, and include oral, topical, and injectable solutions. Cydectin Pour On is a trade name for a formulation for use on cattle and red deer.

Ethyl oleate, a fatty acid ester produced through the condensation of oleic acid and ethanol, serves as the liquid lipid component in nanostructured lipid carriers (NLCs). These NLCs represent a pioneering approach for the oral administration of trans-Ferulic acid (TFA), highlighting ethyl oleate's critical role in enabling effective drug delivery systems.

Buformin hydrochloride (NSC-528218) is a potent AMPK activator,an oral antidiabetic drug of the biguanide class. Buformin delays the absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake into cells and inhibits synthesis of glucose by the liver. Biguanides may antagonize the action of glucagon, thus reducing fasting glucose levels.

(2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal hydrochloride (D-Mannosamine hydrochloride) is a pharmaceutical compound used in the development of mannosylated liposomes for bioadhesive oral drug delivery via M cells of Peyer's patches.

Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

AGI-026 (AGI-12026) is a novel and potent dual inhibitor of the mutant isocitrate dehydrogenase mIDH1/2 with the advantages of oral administration and penetration of the blood-brain barrier, with a drug concentration to plasma concentration ratio (brain/plasma ratio) of 1.5 in brain tissue, and the ability to reduce the accumulation of the carcinogenic metabolite d-2-hydroxyglutarate (2-HG), which is used in the study of mIDH gliomas.

Trifluridine tipiracil hydrochloride mixture (TAS-102) is a novel oral combination drug containing trifluridine (TFT) and tipiracil hydrochloride (TTP) in a 2:1 molar ratio.

Bicyclol (SY801)(SY 801) is an anti-hepatitis drug. Oral administration of bicyclol normalizes the elevated serum transaminases (ALT, AST) by 50% in chronic viral hepatitis B and C, and also has a certain level of inhibiting HBV and HCV replication. In combination therapy of bicyclol with interferon alpha, lamivudine and adefovir dipivoxil in HBV or HCV, bicyclol may reduce YMDD mutant and side effects and increase the anti-viral efficacy.

Miltefosine (HePC) is the treatment of visceral and cutaneous leishmaniasis drug , and is proceeding clinical trials for this in several countries. Several medical agents produce some potency against visceral or cutaneous leishmaniasis, however a 2005 survey concluded that miltefosine is the only effective oral treatment for both forms of leishmaniasis.

CWHM-1008 is an effective oral antimalarial drug. The EC50 values of the drug-sensitive Plasmodium falciparum 3D7 and drug-resistant Dd2 strains are 46 and 21 nM, respectively.

CNDAC, a nucleoside analog, is a major metabolite of oral drug sapacitabine.

Pracinostat (SB939) is a novel HDAC inhibitor with improved in vivo properties compared to other HDAC inhibitors currently in Clinicalal trials, allowing oral dosing. Data demonstrate that Pracinostat is a potent and effective anti-tumor drug with potential as an oral therapy for a variety of human hematological and solid tumors.

(R)-Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) that exhibits oral activity and analgesic properties. Unlike its counterpart, (R)-Ketoprofen does not significantly enhance the increase of inflammatory cytokines (such as Tumor Necrosis Factor (TNF) and Interleukin-1 (IL-1)) induced by LPS. However, it can inhibit the anti-inflammatory activity of (S)-Ketoprofen.

AR antagonist 9 is an orally active, selective androgen receptor (AR) antagonist that inhibits cancer by disrupting the formation of AR ligand-binding domain dimers, showing potential in overcoming drug resistance in prostate cancer (PCa). Its antagonistic activity against AR has an IC50 of 0.051 μM, comparable to Enzalutamide (IC50= 0.060 μM). This compound demonstrates superior inhibitory effects on ARF876L T877A and ARW741C mutants compared to Enzalutamide. Additionally, AR antagonist 9 possesses favorable pharmacokinetic properties, with an oral bioavailability (F) of 66.24% in rats, and significantly inhibits tumor growth in LNCaP xenograft mouse models upon oral administration. AR antagonist 9 holds promise for research in overcoming PCa resistance.

Mtb-IN-10 (Compound P15) is an Rv1625c Cya activator that influences the growth of Mycobacterium tuberculosis (Mtb) by modulating cAMP metabolism. It demonstrates an anti-tuberculosis activity with an EC50 of 1.96 µM in Mtb-infected macrophage models and achieves an oral bioavailability of 58.0% when administered orally to mice at 20 mg kg. Mtb-IN-10 potentially regulates intracellular signaling and disrupts cholesterol metabolism within Mtb, thereby inhibiting bacterial proliferation. It holds promise for tuberculosis (TB) research, particularly targeting multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains of Mtb.

Buformin (1-butylbiguanide) is an oral antidiabetic drug of the biguanide class. It also inhibits the synthesis of glucose by the liver. Buformin delays absorption of glucose from the gastrointestinal tract increases insulin sensitivity and glucose uptake

LY3104607 is a G Protein-Coupled Receptor 40 agonist. It is active in oral treatment for patients with type 2 diabetes mellitus and is a glucose-lowering drug candidate.

PD 130908 is an analogue of RSU 1069 with effective hypoxic cytotoxin, but less potent than RSU 1069. Toxicity toward hypoxic tumor cells in vivo is demonstrated by clamping tumors (for 60 min) following administration of PD 130908. Systemic toxicity is s

SU-13197 is an antiarrhythmic drug with oral activity.

(-) -Mdo-NPA HCl is an oral effective long-acting drug that is active against central dopamine receptors and the similar apophin.

Avitinib (AC0010), also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with potential antineoplastic activity. Upon oral administration, avitinib covalently binds to and inhibits the activity of mutant forms of EGFR, including the drug-resistant T790M EGFR mutant, which prevents signaling mediated by mutant forms of EGFR. This may both induce cell death and inhibit tumor growth in EGFR-mutated tumor cells. EGFR, a receptor tyrosine kinase that is mutated in a variety of Ys, plays a key role in tumor cell proliferation and tumor vascularization. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced when compared to non-selective EGFR inhibitors, which also inhibit wild-type EGFR.

Epelsiban Besylate is an oral drug that is a highly selective anamol oxytocin receptor antagonist.