Osimertinib(AZD-9291) powder

Osimertinib(AZD-9291) powder is an oral, irreversible inhibitor of epidermal growth factor receptor (EGFR) sensitizing and T790M resistance mutations (IC50s = 15-17 nM) while sparing the wild-type form of the receptor (IC50 = 480 nM).1 It binds the related IGF1R And hERG receptors with reduced implantency (IC50s = 2.9 and 16.2 μM, respectively).1 AZD 9291 has been shown to inhibit tumor growth in a xenograft mouse model at oral doses of 5-10 mg/kg and has been tested clinically in patients With advanced EGFR mutant non-small-cell lung cancer.

       

Product Description

 

Osimertinib(AZD-9291) powder video

 

 


 

I.Osimertinib(AZD-9291) powder basic Characters:

 

Name: Osimertinib(AZD-9291) powder
CAS: 1421373-65-0
Molecular Formula: C28H33N7O2
Molecular Weight: 499.61
Melt Point: >188ºC
Storage Temp: -20°C
Color: Light yellow solid powder

 


 

II. AZD-9291 powder in usage:

 

1.Name:

AZD-9291 powder, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide

 

2.AZD-9291 Powder usage:

AZD-9291 powder administered once daily orally at 5 mg/kg caused profound regression of tumours across EGFRm+ (PC9; 178% growth inhibition) and EGFRm+/T790M (H1975; 119% growth inhibition) tumour models in vivo,
after 14 days dosing. Furthermore 5 mg/kg AZD-9291 powder was sufficient to cause significant shrinkage of EGFRm+ and EGFRm+/T790M transgenic mouse lung tumours. Tumour growth inhibition was associated with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK. Chronic long-term treatment of PC9 and H1975 xenograft tumours with AZD-9291 powder led to a complete and sustained macroscopic response, with no visible tumours after 40 days dosing, and being maintained beyond 100 days. Furthermore, pre-clinical data also indicates that AZD-9291 powder could target tumours that have acquired resistance to the more recently identified HER2-amplification mechanism, thus potentially extending its benefit in TKI resistant patients.

 

3.Warning on AZD-9291 powder:

AZD-9291 powder is the only approved medicine indicated for patients with metastatic EGFR T790M mutation-positive non-small cell lung cancer. This indication is approved under the FDA’s accelerated approval process based on tumour response rate and duration of response (DoR).

The common dverse effects include diarrhea, stomatitis, rashes, dry or itchy skin, infections where finger or toenails abut skin, low platelet counts, low leukocyte counts, and low neutrophil counts.
There are no contraindications for TAGRISSO
Interstitial Lung Disease (ILD)/Pneumonitis occurred in 3.3% and were fatal in 0.5% of 813 TAGRISSO patients. Withhold TAGRISSO and promptly investigate for ILD in any patient presenting with worsening of respiratory symptoms indicative of ILD (e.g., dyspnea, cough and fever). Permanently discontinue TAGRISSO if ILD is confirmed
QTc interval prolongation occurred in TAGRISSO patients. Of the 411 patients in two Phase II studies, one patient (0.2%) was found to have a QTc greater than 500 msec, and 11 patients (2.7%) had an increase from baseline QTc greater than 60 msec. Conduct periodic monitoring with ECGs and electrolytes in patients with congenital long QTc syndrome, congestive heart failure, electrolyte abnormalities, or those who are taking medications known to prolong the QTc interval. Permanently discontinue TAGRISSO in patients who develop QTc interval prolongation with signs/symptoms of life threatening arrhythmia
Cardiomyopathy occurred in 1.4% and were fatal in 0.2% of 813 TAGRISSO patients. Left Ventricular Ejection Fraction (LVEF) decline >10% and a drop to <50% occurred in 2.4% of (9/375) TAGRISSO patients. Assess LVEF before initiation and then at 3 month intervals of treatment. Withhold TAGRISSO if ejection fraction decreases by 10% from pretreatment values and is less than 50%. For symptomatic congestive heart failure or persistent asymptomatic LV dysfunction that does not resolve within 4 weeks, permanently discontinue TAGRISSO.
Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during TAGRISSO treatment and for 6 weeks after the final dose. Advise males with female partners of reproductive potential to use effective contraception for 4 months after the final dose.
The most common adverse reactions (>20%) observed in TAGRISSO patients were diarrhea (42%), rash (41%), dry skin (31%) and nail toxicity (25%).

 

4.Further instructions:

AZD-9291 powder was highly active in patients with lung cancer with the EGFR T790M mutation who had had disease progression during prior therapy with EGFR tyrosine kinase inhibitors.

AZD-9291 powder is being studied in the confirmatory trial, AURA3, an open label, randomised Phase III study designed to assess the efficacy and safety of AZD-9291 powder versus platinum-based doublet chemotherapy in patients with EGFR T790M positive, locally advanced, or metastatic NSCLC who have progressed following prior therapy with an EGFR-TKI. AZD-9291 powder is also being investigated in the adjuvant setting and in the metastatic first-line setting, including in patients with brain metastases, as well as in combination with other compounds.

AZD-9291 powder 80mg once-daily tablet is the first medicine indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small-cell lung cancer (NSCLC), as detected by an FDA-approved test, who have progressed on or after EGFR tyrosine kinase inhibitor (TKI) therapy. Non-clinical in vitro studies have demonstrated that AZD-9291 powder has high potency and inhibitory activity against mutant EGFR phosphorylation across the range of clinically relevant EGFRm and T790M mutant NSCLC cell lines with significantly less activity against EGFR in wild-type cell lines.

Osimertinib powder has recently been published by the World Health Organisation (WHO) as the proposed International Non-proprietary Name (INN) for AZD-9291 powder, and may become formally adopted during November 2015. In the US, the American Medical Association accepted Osimertinib powder as the United States Adopted Name (USAN).

 

5. AZD-9291 Powder:

Min order 10grams.
The inquiry on normal quantity(Within 1kg) can be sent out in 12 hours after payment.
For larger order(Within 1kg)can be sent out in 3 workingdays after payment.

 

6. Caffeic Acid Phenethyl Ester Powder Recipes:

To inquiry our Customer Representitive(CSR) for details, for your reference.

 

7. Caffeic Acid Phenethyl Ester Marketing:

To be provided in the coming future.

 


 

III. AZD-9291 powder HNMR

 

 

 


 

IV. How to buy Osimertinib powder; buy AZD-9291 powder from AASraw?

 

1.To contact us by our email inquiry system,or online skypecustomer service representative(CSR).
2.To provide us your inquired quantity and address.
3.Our CSR will provide you the quotation, payment term, tracking number, delivery ways and estimated arrival date(ETA).
4.Payment done and the goods will be sent out in 12 hours(For order within 10kg).
5.Goods received and give comments.

 


 

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