elimination

PLX5622 is a highly selective, brain-penetrant, and orally active CSF1R inhibitor.

BNTA is a potent extracellular matrix (ECM) modulator. In a rat model of arthritis, BNTA modulates arthritis by promoting the synthesis of cartilage structural molecules on chondrocytes through the induction of superoxide dismutase 3 (SOD3) and regulating chondrogenesis through superoxide anion elimination.

TP-16 is a novel potent and selective EP4 antagonist that blocks the function of IMCs and enhances cytotoxic T cell-mediated tumor elimination in vivo.

Atracurium besylate (51W89) is a non-depolarizing neuromuscular blocking agent with short duration of action. Its lack of significant cardiovascular effects and its lack of dependence on good kidney function for elimination provide clinical advantage over alternate non-depolarizing neuromuscular blocking agents.

Fosfomycin calcium (Phosphomycin calcium salt) is a blood-brain barrier penetrating, broad-spectrum antibiotic by irreversibly inhibiting an early stage in cell wall synthesis.

D-Glucuronic acid sodium salt monohydrate (Sodium D-glucuronate) is a carboxylic acid that is highly soluble in water. In humans, glucuronic acid often binds to toxic substances to facilitate elimination and to hormones to aid in their transport.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

2-Quinolinecarboxaldehyde (Quinoline-2-carbaldehyde) is a small rigid molecule that is a compound in the Henry reaction and subsequent elimination. 2-Quinolinecarboxaldehyde inhibits AChE with an IC50 of 13.48 μM.

Secnidazole (PM-185184) is a second-generation 5-nitroimidazole antimicrobial that is structurally related to other 5-nitroimidazoles including [DB00916] and [DB00911], but displays improved oral absorption and longer terminal elimination half-life than antimicrobial agents in this class [A27210]. Secnidazole is selective against many anaerobic Gram-positive and Gram-negative bacteria and protozoa.

Disodium succinate (Sodium succinate) is the sodium salt form of succinate, which is an important metabolite at the cross-road of several metabolic pathways and involved in the formation and elimination of reactive oxygen species.

Hexaflumuron is a chitin synthesis inhibitor used to bait and eliminate termite colonies. Termites are unable to metabolize hexaflumuron and clearance is slow, resulting in up to 100% elimination. Hexaflumuron has also been tested for use with the raisin

Fosfomycin sodium is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria, including multidrug-resistant Gram-negative bacteria, by irreversibly inhibiting an early stage in cell wall synthesis.

D-Phenothrin ((-)-trans-Phenothrin) is a type II synthetic pyrethroid extensively employed in veterinary medicine for pest control on animals, crop protection, and the elimination of insects, mosquitoes, and human lice.

Meproscillarin is a glycoside with high bioavailability (about 70%) and an elimination independent of renal function.

Dasiglucagon acetate is a novel glucagon analog for diabetic hypoglycemia therapy. Dasiglucagon acetate has demonstrated established solubility and stability in an aqueous formulation. Pharmacokinetics studies have shown dasiglucagon acetate to exhibit hi

An antibiotic produced by Streptomyces fradiae.

Etebenecid (Urelim) is uricosuric agents, which lower uric acid levels in the body by increasing the elimination of uric acid by the kidneys. It also inhibits penicillin tubular secretion.

IU1-47 is an effective and specific USP14 inhibitor (IC50: 0.6 μM). IU1-47 causes tau elimination in cultured neurons. IU1-47 inhibits IsoT/USP5 (IC50: 20 μM).

Spirorenone is an androstadienone derivative as a highly effective aldosterone antagonist. Spirorenone is 8.6 times as potent as spironolactone, but showed a lower affinity for the mineralocorticoid receptors. In phase I clinical trials Spirorenone was absorbed with a half-life of 20-30 min, achieving maximum concentrations of about 100 ng/ml (10 mg) and 260 ng/ml (40 mg) after 1-2 h. Disposition of the parent drug was biphasic with half-lives of 50-60 min (distribution) and 5-6 h (elimination). Neither significant accumulation nor enzyme induction was observed after prolonged treatment.

Paromomycin (Sulfate Salt) is an aminoglycoside that is active against Gram-negative and many Gram-positive bacteria as well as some protozoa and cestodes. Paromomycin in combination with sodium stibogluconate has proven to be effective in African and Indian VL (visceral leishmaniasis) and improves survival in African VL[3]. PS (Paromomycin Sulfate) is effective for elimination of B. coli without hematological side effects[4]. The activity of phosphoglucose isomerase was slightly inhibited by 10(-3) M paromomycin sulfate while those of hexokinase, phosphofructokinase and glucose-6-phosphate dehydrogenase were not inhibited[5]. In addition, with regard to correlation of endotoxemia with renal impairment, endogenous creatinine clearance and p-aminohippurate clearance were significantly improved (P less than 0.02) in those patients whose endotoxemia disappeared on paromomycin sulfate administration. Paromomycin sulfate seems to be effective in the prevention of endotoxemia and the associated renal impairment in cirrhosis in man[6]. Significantly higher frequencies of resistance to paromomycin, kanamycin, neomycin and tobramycin were observed in S. aureus isolates from PS (paromomycin supplemented) birds. Paromomycin supplementation resulted in resistance to aminoglycosides in bacteria of PS turkeys. Co-selection for resistance to other antimicrobial agents was observed in E. coli isolates[7].

Dusquetide (SGX942) TFA, a first-in-class innate defense regulator (IDR), modulates the innate immune response to pathogen-associated molecular patterns (PAMPs) and damage-associated molecular patterns (DAMPs) by interacting with p62. This compound is effective in both diminishing inflammation and enhancing the elimination of bacterial infections [1].

Clinodiside A in rats with one compartment open model into the body, rapid distribution, elimination rate.

Sotrovimab (VIR 7831), a human IgG1κ pan-sarbecovirus monoclonal antibody (mAb), effectively neutralizes SARS-CoV-2, SARS-CoV-1, and various other sarbecoviruses. Developed from S309, it possesses a prolonged half-life and excellent bioavailability within the respiratory mucosa. Its mechanism potentially facilitates immune-mediated viral elimination, thereby averting the advancement of Covid-19 during the disease's early stages [1][2].

Poly(acrylic acid) serves as an effective corrosion inhibitor for pure cast aluminium in acidic environments through its adsorption onto the metal's surface. Additionally, this compound functions as an excipient within the pharmaceutical industry, utilized in roles such as a coating material and release blocker. Pharmaceutical excipients, also known as pharmaceutical auxiliaries, are chemical substances employed in drug formulation alongside the active pharmaceutical ingredients to enhance the stability, solubility, and manufacturability of the products. These excipients also influence the absorption, distribution, metabolism, and elimination (ADME) processes of drugs [1] [2].

Polyoxyethylene Sorbitan Monostearate, an ester derived from the saturated fatty acid stearic acid (C18:0), serves multiple roles in pharmaceutical formulations, including as a surfactant, emulsifier, solubilizer, and wetting agent. As a pharmaceutical excipient—an inert substance that enhances the stability, solubility, and processability of drug formulations—it plays a crucial role in affecting the absorption, distribution, metabolism, and elimination (ADME) processes of drugs [1] [2].

Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a chemically synthesized E3 ligase ligand-linker conjugate, incorporating the cereblon ligand from Pomalidomide and a linker used in PROTAC technology. It facilitates targeted protein degradation by modulating E3 ligase activity, thereby enabling the selective elimination of specific proteins of interest.

Crocin II (Crocetin gentiobiosylglucosyl ester) has anti-inflammatory and anti-apoptotic effects against gastric ischemia-reperfusion injury in rats, the effect of crocin is mainly mediated by reducing the protein expression of iNOS and caspase-3. Crocin II can ameliorate CCl4-induced liver injury via inhibition of inflammatory cytokines, caspase3 and oxidative stress along with modulation of liver metabolizing enzymes favoring elimination of CCl4 toxic metabolite. Crocin II has antihyperlipidemic effect, may be due to the inhibition of pancreatic lipase and crocin, and its metabolite, Crocin II , can improve hyperlipidemia. Crocin has antidepressant effects by increasing CREB, BDNF and VGF levels in hippocampus.

Tidutamab (XmAb-18087) is a humanized, affinity-optimized bispecific antibody (bsAb) targeting the SSTR2 and CD3 domains to bind somatostatin receptor 2 (SSTR2) and T cells, respectively. Featuring a full Fc domain for extended serum half-life, it engages in the targeted elimination of SSTR2-positive tumor cells via redirected T cell-mediated cytotoxicity (RTcC) [1].

PLX5622 hemifumarate is a highly selective, brain-penetrant, and orally active CSF1R inhibitor with an IC50 of 0.016 μM and Ki of 5.9 nM. It allows for extended and specific microglial elimination preceding and during pathology development and demonstrates desirable PK properties in various animals [1] [2].

Desmethylazelastine, the primary active metabolite of Azelastine, undergoes oxidative metabolism via the cytochrome P450 enzyme system, exhibits a 97% protein binding rate, and has an elimination half-life of 54 hours. Azelastine, an orally active, selective, and high-affinity histamine H1-receptor antagonist, is utilized in the research of allergic rhinitis, asthma, diabetic hyperlipidemia, and SARS-CoV-2 [1] [2] [3] [4] [5].

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012) 2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)

Acenocoumarol is a short-lived oral anti-coagulant, which, like warfarin, functions by inhibiting vitamin K epoxide reductase. It has higher intrinsic anticoagulant potency than warfarin and phenprocoumon, when evaluated in vitro. Acenocoumarol has a single chiral center that gives rise to two different enantiomeric forms. (S)-Acenocoumarol has a shorter plasma elimination half-life (1.8 hours) and faster plasma clearance (28.5 L/hour), compared to the (R)-enantiomer (6.6 hours, 1.9 L/hour). The S-enantiomer undergoes extensive first-pass metabolism during absorption from the gastrointestinal tract, whereas (R)-acenocoumarol is rapidly absorbed and provides essentially complete oral bioavailability. Perhaps related to these pharmacokinetic characteristics, (S)-acenocoumarol is less potent in vivo as an anti-coagulant than the (R)-enantiomer. As the clearance of acenocoumarol is ~20-fold faster than that for warfarin, the plasma concentrations of acenocoumarol are substantially lower than those for warfarin in patients receiving long-term treatment.

PROTAC BRD2 BRD4 degrader-1 (compound 15) is a potent, selective degrader of BET proteins BRD4 and BRD2, achieving rapid, reversible, and unexpectedly selective elimination compared to BRD3. It effectively suppresses solid tumors with minimal cytotoxic effects and comprises a BET inhibitor, a connecting linker, and thalidomide as the ligand for cereblon (CRBN) cullin 4A[1].

Vibecotamab (XmAb14045) is a potent bispecific antibody that targets CD123 and CD3, promoting T cell-mediated elimination of CD123-expressing cells. It exhibits antitumor properties and is used in studies on acute myeloid leukemia [1].

Arbaclofen placarbil( XP19986) is a GABA(B) receptor agonist.Arbaclofen Placarbil is a novel R-baclofen prodrug with improved absorption, distribution, metabolism, and elimination properties compared to R-baclofen. And it can reduce postprandial reflux in

BMS-962212, a direct, reversible, and selective factor XIa (FXIa) inhibitor, demonstrates fast pharmacodynamic (PD) response onset and rapid elimination with a well-tolerated profile. It dependently increases activated partial thromboplastin time and decreases FXI clotting activity exposure [1].

Cellulose can be used as an excipient. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs [1] .

LS-BF1, a stable and low-toxicity cationic antimicrobial peptide, exhibits broad-spectrum antibacterial activity that encompasses the notorious ESKAPE pathogens through a cell membrane disruption mechanism. The compound demonstrates effective in vivo bacterial elimination in a mouse infection model[1].

Maltodextrin (dextrose equivalent 16.5-19.5) serves as an excipient in pharmaceutical applications. Excipients, also known as pharmaceutical auxiliaries, are chemical substances utilized in drug formulation alongside active pharmaceutical ingredients. They primarily enhance the stability, solubility, and processability of drug preparations, while also influencing the absorption, distribution, metabolism, and elimination (ADME) of co-administered drugs [1].

UR-7247 is an angiotensin type 1 receptor antagonist with a very long plasma elimination half-life.

AFN-1252, also known as AFN-12520000; API-1252; Debio-1452, is FASII Inhibitor which is potentially for the treatment of acute bacterial skin. AFN-1252 exhibits typical MIC(90) values of ≤0·015 μg/ml against diverse clinical isolates of S. aureus, oral absorption, long elimination half-live and efficacy in animal models. AFN-1252 efficiently blocked daptomycin-induced phospholipid decoy production, even in the case of isolates resistant to AFN-1252, which prevented the inactivation of daptomycin and resulted in sustained bacterial killing. In turn, daptomycin prevented the fatty acid-dependent emergence of AFN-1252-resistant isolates in vitr

L-Methionine γ-lyase (Methionine lyase), a multifaceted enzyme in the γ-family of pyridoxal-5’-phosphate (PLP)-dependent enzymes, catalyzes the α, γ-elimination of L-methionine and homocysteine. This enzyme exhibits anticancer and anti-infectious properties and is utilized in homocysteinemia research [1][2][3].

Trisodium phosphate dodecahydrate serves as a corrosion inhibitor for iron in 0.1 M NaClO4 solutions, effective under both aerated and deaerated conditions. Additionally, it acts as an excipient in pharmaceutical formulations, functioning primarily as a pH regulator and buffer. These excipients, also known as pharmaceutical auxiliaries, are substances utilized in the pharmaceutical manufacturing process besides the active pharmaceutical ingredients. They are crucial for enhancing the stability, solubility, and processability of pharmaceutical products. Moreover, pharmaceutical excipients play a significant role in influencing the absorption, distribution, metabolism, and elimination (ADME) of co-administered drugs, thereby affecting their efficacy and safety [1] [2].