What is Aprepitant?
Aprepitant powder is white or slightly white crystal powder, which is a chemical substance and insoluble in water. The solubility of aripipitan in water is very low at pH 2 ~ 10, with a Log P of 4.8 at pH 7.0. Slightly soluble in acetonitrile, slightly soluble in ethanol and isopropyl acetate, soluble in ethanol.
Aprepitant is a Neurokinin-1(NK-1) receptor antagonist, which belongs to the anti-cancer chemotherapy and vomiting treatment products. Aprepitant has high selective affinity for human, but low affinity for 5- hydroxytryptamine, dopamine and corticosteroid receptors. Substance P is a kind of tachykinin (neurokinin), which is mainly located in central and peripheral nervous system neurons. It is related to many functions, such as vomiting, depression, inflammatory pain and inflammation of other diseases. The action of substance P is mediated by NK-1 receptor, which is a G protein receptor and coupled with phosphoinositide signal pathway. Aprepitant binds to NK-1 receptor in the brain and blocks the receptor, thus treating diseases mediated by substance P. Aprepitant can selectively prevent the combination of substance P and NK-1 receptor in the central nervous system to stop vomiting, and can be used for nausea and vomiting caused by moderate and high emetic chemotherapy drugs.
| Product name | Aprepitant |
| CAS | 170729-80-3 |
| Molecular formula | C23H21F7N4O3 |
| Molecular weight | 534.43 |
| EINECS Number | 677-636-6 |
| Storage condition | Sealed in dry,2-8°C |
| Melting point | 244-246°C |
| Solubility | Soluble in DMSO(>25mg/ml) |
| Appearance | White to beige powder |
| Specific Rotation | D25 +69° (c = 1.00 in methanol) |
| Density | 1.51±0.1 g/cm3(Predicted) |
What is the pharmacological action of Aprepitant?
It blocks the action of substance P by binding to NK-1 receptor, which mainly exists in the central nervous system and its periphery. Aprepitant powder can occupy NK-l receptors in the brain through the blood-brain barrier, with high selectivity and affinity, but low affinity for NK-2 and NK-3 receptors. At the same time, the affinity of Aprepitant to the targets of other drugs (such as dopamine receptor and 5-HT3 receptor) used to treat nausea and vomiting induced by chemotherapy is also very low, and its effect of reducing nausea and vomiting is better than other drugs. This product can improve the complete response rate of acute and delayed nausea and vomiting induced by chemotherapy in the standard method of treating severe vomiting symptoms caused by chemotherapy with 5- tryptamine 3(5-HT3) receptor blocker and dexamethasone. Aprepitant can inhibit acute and delayed vomiting induced by Cisplatin in the white helper animal model. Single dose before or at the same time with cisplatin. Aprepitant can reduce vomiting symptoms in the next 72 hours; At the same time, Aprepitant can also enhance its antiemetic effect by combining with dexamethasone or 5-HT and receptor blocker ondansetron.
Product Specification
| Item | Specification | Results |
| Appearance | White or off-white crystalline powder | White solid powder |
| Identification | By IR | Complies |
| By HPLC | Complies | |
| Solu bility | Freely soluble in dimethyl sulfoxide,insoluble in water |
Complies |
| Specific Rotation | +66.0~+71.0° | +67.0° |
| Water Content | ≤0.50% | 0.13% |
| Loss on Drying | ≤0.50% | 0.10% |
| Residue on Ignition | ≤0.10% | 0.06% |
| Organic Impurities | Impurity AP0:≤0.15% | ND |
| Impurity AP1:≤0.15% | ND | |
| Impurity AP2:≤0.15% | ND | |
| Desfluoro aprepitant:≤0.15% | ND | |
| Any other individual impurity:≤0.10% | 0.06% | |
| Total Impurities:≤0.30% | 0.25% | |
| Assay | 98.0%~102.0% | 99.85% |
| Conclusion: | Conform with enterprise specification. |
What are the functions of Aprepitant?
Aprepitant powder is an anti-tumor auxiliary drug with antiemetic, anti-inflammatory, anticoagulant, antioxidant, and gastrointestinal function improvement effects and functions.
1. Antiemetic:
Aprepitant can inhibit acute and delayed vomiting caused by cisplatin, and enhance the antiemetic activity of 5-HT3 receptor antagonist ondansetron and glucocorticoid dexamethasone on vomiting caused by cisplatin. Therefore, Aprepitant can be used to relieve nausea and vomiting symptoms.
2. Anti-inflammatory:
Aprepitant has a certain anti-inflammatory effect, which can inhibit the proliferation of granulation tissue and eliminate inflammatory response. This has a relieving effect on the inflammatory symptoms that may occur in tumor patients during treatment.
3. Anticoagulant:
Aprepitant has a certain anticoagulant effect and can reduce blood viscosity. High viscosity can lead to microcirculatory disorders, and the anticoagulant effect of aprepitant capsules helps improve microcirculation.
4. Antioxidant:
Aprepitant has the effect of scavenging free radicals, and can reduce oxidative stress by capturing free radicals.
5. Improve gastrointestinal function: Aprepitant can increase gastrointestinal blood supply, reduce gastric acid secretion, and improve gastrointestinal function.
HTML5 atlas of Aprepitant
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What is the difference between fosaprepitant and aprepitant?
1. Product ingredients and main effects
Fosaprepitant is mainly used as an antiemetic drug and has anti-tumor effects. It can be used to treat recurrent brain metastases by enhancing angiogenesis in tumor tissue and increasing the antigenicity of tumor tissue, thereby achieving an anti-tumor effect. Aprepitant powder is an anti-tumor adjuvant drug, mainly used to prevent acute and delayed nausea and vomiting during the initial and repeated treatment of highly emetogenic anti-tumor chemotherapy.
2. Mechanism of action
Fosaprepitant acts on tumor tissue through its specific mechanism of action, which may include affecting the growth and metastasis of tumor cells. Aprepitant mainly inhibits the 5-hydroxytryptamine receptors in neurons to inhibit the excitability of neurons for anti-tumor treatment, and is administered in combination with other antiemetic drugs to prevent nausea and vomiting caused by chemotherapy.
Biological Activity of Aprepitant：
| Describe | Aprepitant is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM. |
| In vitro studies | Aprepitant reduces metabolic activity with an estimated IC50 value of 20μM. Aprepitant induces cell growth inhibition and G1 cell cycle arrest. Aprepitant significantly induces apoptosis in Nalm-6 cells, which is mediated through caspase-3 activation. Aprepitant (20μM) induces p53 accumulation and expression of pro-apoptotic p53 target genes. Aprepitant (1, 5, 10μM) inhibits HIV infection in MDM from depressed and unsuppressed HIV-negative individuals ex vivo in a dose-dependent manner. The IC90 value of aprepitant is equivalent to 10μM and the IC50 value is approximately 5μM. |
| In vivo studies | Aprepitant prevents B. burgdorferi infection-induced increase in NK-1R expression in NHPs in vivo. Aprepitant treatment prevents B. burgdorferi-induced increase in CCL2 protein levels in the cerebrospinal fluid of NHPs. Aprepitant treatment prevents B. burgdorferi-induced increase in CCL2 and CXCL13 mRNA expression in dorsal root ganglia of NHPs and prevents B. burgdorferi-induced increase in CCL2, CXCL13, IL-17A, and IL-6 mRNA expression in the spinal cord of NHPs. Aprepitant treatment attenuates B. burgdorferi infection-induced decrease in astrocyte activity/number. Aprepitant (10 mg/kg, ip) significantly attenuates AMPH- and cocaine-induced CPP expression and locomotor activation in mice. In contrast, aprepitant significantly enhances morphine-induced CPP expression while significantly inhibiting morphine-mediated locomotor activity in mice. Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or inhibition. Aprepitant (125 mg/day, orally) resulted in a 1-log reduction in plasma levels of viral RNA compared to untreated controls. |
| Cell experiments | The inhibitory effect of aprepitant on the metabolic activity of Nalm-6 cells was evaluated by the uptake of thiazolyl blue tetrazolium bromide (MTT) by living cells. Cells were seeded onto 96-well plates at a density of 5000 cells/well. After treatment with 5, 10, 15, 20, and 30 μM of aprepitant for 24, 36, and 48 h, the cells were further incubated with 100 μM MTT (0.5 mg/mL) at 37 °C for 3 h. Untreated cells were defined as the control group. After solubilization of the precipitated formazan with 100 μL DMSO, the optical density was measured at a wavelength of 578 nm using an ELISA reader. |
| Animal experiments | Fifteen rhesus monkeys were anesthetized and inoculated intrathecally into the cisterna magna with 1 × 108 viable spirochetes, whereas 5 rhesus monkeys were uninfected and received 1 mL of RPMI 1640 medium after removal of an equal amount of CSF. Establishment of in vivo B. burgdorferi infection was confirmed by positive culture from at least one autopsy tissue sample. The first group of animals was studied for 2 weeks and included two control animals (one of which was treated with aprepitant), two infected and untreated animals, and two infected animals treated with aprepitant. The second group of animals was studied for 4 weeks and included 3 control animals (one of which was treated with aprepitant), 5 infected and untreated animals, and 4 infected animals treated with aprepitant. Animals received a mean daily dose of aprepitant of 28 ± 6 mg/kg per day, and drug treatment was initiated 2 days prior to inoculation. These doses are consistent with standard veterinary protocols for selected drugs in NHPs, and the 4-week duration of the study precludes the development of neuropathology that occurs 8 weeks after B. burgdorferi infection. |
| References |
[1]. Martinez AN, et al. Aprepitant limits in vivo neuroinflammatory responses in a rhesus model of Lyme neuroborreliosis. J Neuroinflammation. 2017 Feb 15;14(1):37. [2]. Bayati S, et al. Inhibition of tachykinin NK1 receptor using aprepitant induces apoptotic cell death and G1 arrest through Akt/p53 axis in pre-B acute lymphoblastic leukemia cells. Eur J Pharmacol. 2016 Nov 15;791:274-283. [3]. Mannangatti P, et al. Differential effects of aprepitant, a clinically used neurokinin-1 receptor antagonist on the expression of conditioned psychostimulant versus opioid reward. Psychopharmacology (Berl). 2017 Feb;234(4):695-705. [4]. Barrett JS, et al. Pharmacologic rationale for the NK1R antagonist, aprepitant as adjunctive therapy in HIV. J Transl Med. 2016 May 26;14(1):148. |
What are the precautions for Aprepitant?
Aprepitant is a dose-dependent CYP3A4 inhibitor and must be used with caution when used with products that are primarily metabolized by CYP3A4; some chemotherapy drugs are metabolized by CYP3A4.
Aprepitant can cause a significant decrease in the international normalized ratio (INR) of the prothrombin time when used with warfarin.
The efficacy of hormonal contraceptives may be reduced during and for 28 days after aprepitant use. Therefore, alternative contraceptive measures or rescue methods should be used for contraception during aprepitant use and for 1 month after the last dose of aprepitant.
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