Tenofovir disoproxil

한글명:Tenofovir disoproxil

카스 번호201341-05-1

상품명:Tenofovir disoproxil

CBNumberCB0949152

분자식C19H30N5O10P

포뮬러 무게519.44

MOL 파일201341-05-1.mol

화학적 성질

끓는 점	642.7±65.0 °C(Predicted)
밀도	1.45±0.1 g/cm3(Predicted)
저장 조건	Keep in dark place,Inert atmosphere,2-8°C
용해도	DMSO: ≥ 38 mg/mL (73.16 mM)
산도 계수 (pKa)	4.20±0.10(Predicted)
물리적 상태	Solid
색상	White to off-white
CAS 데이터베이스	201341-05-1

Tenofovir disoproxil 화학적 특성, 용도, 생산

개요
Tenofovir disoproxil is a prodrug in a manner similar to that of adefovir dipivoxil. In both cases, the phosphate esters are removed through the action of plasma esterase, leading in this case to tenofovir, which differs from adefovir by the presence of the indicated methyl group. Tenofovir disoproxil exhibits good bioavailability (25%), which is improved in the presence of food (35%). The drug is approved for the treatment of HIV infections in adult patients. Tenofovir diphosphate is an HIV RT inhibitor. The active form of tenofovir is the tenofovir diphosphate, which competes with dATP for incorporation into viral DNA, and when incorporated, tenofovir diphosphate results in premature termination of DNA growth and inhibition of DNA polymerase. Tenofovir disoproxil is indicated for treatment-experienced patients with HIV-1. The drug also appears to be effective in treatment-naive patients, but initial approval is for treatment-experienced patients. The drug is administered as one tablet taken once daily. It is recommended that the drug be combined with other RT inhibitors or HIV PIs, which results in additive or synergistic activity.
용도
Tenofovir Disoproxil is a therapeutic option for nucleos(t)ide analog (NA)-experienced chronic hepatitis B (CHB) patients infected with hepatitis B virus (HBV). Also, it is an intermediate used in the synthesis of Tenofovir Disoproxil Dimer (T018515), which is a Tenofovir Disoproxil impurity.
정의
ChEBI: An organic phosphonate that is the disoproxil ester of tenofovir. A prodrug for tenofovir, an HIV-1 reverse transcriptase inhibitor, tenofovir disoproxil is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.
일반 설명
Tenofovir disoproxil is a prodrug analogously with abacavir.Plasma and tissue esterases cleave the phosphateprotecting groups, releasing the active drug. The bioavailabilityof tenofovir is about 35% when administered withfood. The drug is approved by the Food and DrugAdministration (FDA) for the treatment of HIV infectionsin adult patients. Recommendations are for the drug to beadministered with other RT inhibitors or PIs to achievesynergism.

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