Hauj lwm lawm

Kev tsis

Lub hauv paus rau phau ntawv

raws

product-1400-1400

Cov khoom lag luam

#### 1. Cov ntaub ntawv yooj yim tshuaj thiab cov khoom siv dag zog

Titemifas citrate, lub npe ua lag luam ** F fereston **, yog ib qho kev xaiv tshuaj estrogen (txuj ci uas tsim nyog Nws cov qauv tshuaj lom tau zoo sib xws rau thawj-tiam tshuaj Tamoxifen, tab sis nws cov kev ua tau zoo thiab kev nyab xeeb tau zoo los ntawm kev hloov kho molecular.

- ** tus lej lej **: 89778-27-8

- ** Cov mis molecular **:: C₂₆₂₆ClnoT · C₆h₈o₇

- ** Molecular hnyav **: 598.09 g / mol

- ** Pom zoo ** ** Dawb rau off-dawb crystalline hmoov

- ** Solubility **: Yooj yim soluble hauv cov kuab tshuaj los ntawm methanol thiab ethanol, solaws me ntsis hauv dej (Bioavailability yuav tsum tau txhim kho los ntawm kev tsim tawm thev naus laus zis).

** Cov txiaj ntsig ** **:

1. Cov tshuaj ruaj khov rau lub sijhawm, tuaj yeem khaws cia ntev nyob rau hauv cov chaw qhuav thiab teeb pom kev zoo;

2. Kas cov txheej txheem synthesis, haum rau cov khoom lag luam loj;

3. Citricqu acid kev sib koom tes txhim kho cov dej solubility, uas yooj yim rau kev tsim qauv.

#### 2. Pharmacological thiab cov ntawv thov kev kho mob

** 1. Mechanism ntawm Kev Ua **

Raws li cov ncauj lus, toremifene coj los khi rau estrogen receptors (ER), tso cov khoom siv ntawm cov kua mis, tiv thaiv cov khoom siv tshuaj estrogen. thiab cov simulates ib feem ntawm cov tshuaj estrogen hauv pob txha thiab cov hlab ntshav kom txo qis kev pheej hmoo ntawm cov txha epeumorosis.

** 2. Qhia tau **

- ** Metastatic mis cancer **: Feem ntau yog siv rau thawj-kab kev kho mob ntawm cov poj niam cancer mis ntawm cov poj niam mob cancer mis.

- ** Kev kho mob ": tiv thaiv kev rov qab ua dua tshiab hauv cov pab pawg muaj kev pheej hmoo;

- ** Kawm qhia txog ": Prostate Cancer, Ovarian Cancer (chaw kho mob theem).

** 3. Pharmacokinins **

- ** ** Ib nrab-lub neej **: Txog 5 hnub (metabolite n-desmethyl toremifene yog nquag);

- ** Metabolic Pathway **: Feem ntau metabolized nyob rau hauv daim siab los ntawm CYP3A4 enzyme system thiab tawm los ntawm bile;

- **Bioavailability**: good oral absorption (>90%), thiab cov khoom noj tsis muaj qhov cuam tshuam tseem ceeb ntawm kev nqus.

** Cov txiaj ntsig ** **:

- Piv nrog Tamoxifen, ** Qhov pheej hmoo ntawm Envometrial Thickening yog txo qis ** thiab kev nyab xeeb yog qhov zoo dua;

- Nws tseem ua tau zoo rau qee qhov tamoxifen-resistant cov neeg mob;

- Siv ntev ntev muaj cov txiaj ntsig tiv thaiv rau cov pob txha ceev.

#### 3. Cov txheej txheem ntau lawm thiab kev tswj hwm zoo

** 1. Synthesis txoj kev **

Cov txheej txheem txheej txheem siv "triphenycyletylene ** Thaum niam txiv tseemceeb thiab yog synthesized los ntawm cov kauj ruam hauv qab no:

1. ** Cov tshuaj ntsuam chlorination **: Qhia cov tshuaj chlorine atoms los txhim kho cov receptor khi;

2. ** Kev tawm tsam amination **: Txuas Sab Saw cov pab pawg los tsim cov laj thawj toremifene;

3. ** Kev ua kom muaj kuab lom **: Hloov kho nrog citric acid kom tsim cov citrate ruaj khov, thiab tom qab ntawd crystallize thiab qhuav kom tau txais cov khoom tiav.

** Cov txuj ci tseem ceeb nyuaj **:

- Kev ua kom huv ntawm cov nruab nrab (impurities xws li CIS-ISOMER cov ntsiab lus yuav tsum tau tswj);

- Tswj cov khoom siv lead ua ntawm cov khoom kawg (cuam tshuam rau solubility thiab tsim kev ua tiav).

** 2. Cov Qauv Zoo **

Raws li ** USP / EP / CHP / CHP / CHP / CHP / CHP / CHP ** Pharmacopoeia, txhais tau tias muaj xws li:

- ** Purity **: HPLC Txujcab pom cov khoom tseem ceeb tshaj lossis sib npaug nrog 99. {2}}%;

- ** EGRISUR Spectrum **: Ib leeg impurity tsawg dua los yog sib npaug rau 0. 5%, tag nrho cov impurity tsawg dua los yog sib npaug rau 1.5%;

- ** Muab cov kuab tshuaj uas muaj me nyuam yaus **: methanol, ethanol, thiab lwm yam. Ntsib Ich Q3C yuav tsum tau ua.

#### 4. Kev ua lag luam thiab daim ntawv thov

** 1. Tsim qauv **

- ** Tablet **: 60 mg / ntsiav tshuaj (mainstream duas daim ntawv, qhov ncauj ib hnub);

- ** Kev txhaj tshuaj **: Kev Tshawb Fawb (rau cov neeg mob uas tsis tuaj yeem coj nws los).

** 2. Chaw Tsim Tshuaj Loj **

- ** Kev Tshawb Fawb Kev Tshawb Fawb Txog Kev Tshawb Fawb **: Orion pharma ntawm Finland (lub npe luam npe fareston);

- ** API tus neeg siv khoom **: Dr. Reddy's Is Nrias teb, Hengru cov tshuaj ntawm Tuam Tshoj, thiab lwm yam;

- ** Cov lag luam tshuaj tsis muaj tseeb **: Tom qab cov kws ua yeeb yaj kiab patent, cov tuam txhab generic cov ntaub ntawv tawm nrawm dua lawv cov txheej txheem.

** 3. Nqe thiab Khw Muag Khoom **

- ** API nqe **: Txog $ 2000-2500 / kg (2023 cov ntaub ntawv);

- ** Focusional Nkag **: European Cones Lwm Tus Thawj Coj, thiab Tebchaws Asia-Pacific muaj kev loj hlob tus nqi (nce kev loj hlob cancer mis).

#### 5. Kev tshawb fawb kev nce qib thiab yav tom ntej cov lus qhia

** 1. Kev txhim kho ntawm cov cim tshiab **

- ** Txiv neej mob cancer mis **: Kev tshawb nrhiav kev kho rau cov kab mob tsawg;

- ** HETRATION-resistant prostate cancer **: Kev kuaj mob kev sim ntawm kev sib koom ua ke Androgen Deprivation Kev Kho Mob (ADT).

** 2. Ua Yeeb Yam Siv Tshuaj **

- ** Ua ke nrog CDK4 / 6 Inhibitors ** (xws li palbociclib) los txhim kho los tiv thaiv kev tawm tsam cov qog;

- ** Ua ke nrog cov tshuaj tiv thaiv kev tiv thaiv kab tiv thaiv kev tiv thaiv kab mob ** txhawm rau tswj lub qog mis microenviror.

** 3. Ntsej Muag Dosage Daim Ntawv Tsim Tawm **

- ** Nanocrystal thev naus laus zis **: Txhim kho qhov ncauj xyoob;

- ** ** Hloov Chaw Nruab Nrab **: Txo cov nyhuv dhau los hauv daim siab thiab txo cov kev mob tshwm sim.

### 6. Kev nyab xeeb thiab kev tswj hwm

** 1. Cov kev sib raug zoo **

- Feem ntau: kub flashes (35%), xeev siab (20%), thiab tawm hws;

- Nyaub Cov Mob Siab: Qt Kev Tshawb Fawb Ntev (ECG kev soj ntsuam), ntuav tsis zoo (qis dua tamoxifen).

** 2. Kev cai hloov pauv dua **

- ** FDA **: Yuav tsum muaj lub thawv dub ceeb toom (thrombosis thiab endometrial cancer muaj kev phom sij);

- ** EMA **: Pom zoo cov kev kuaj mob gynecological tsis tu ncua;

- ** Tuam Tshoj NMPA **: suav nrog cov ntaub ntawv ua ntej (rau cov ntaub ntawv ntau dua tshiab).

### cov ntsiab lus

Titemifas citrate, raws li ib qho tshuaj tseem ceeb rau kev kho mob cancer mis, txuas ntxiv mus rau kev ua lag luam nrog nws qhov kev tsim nyog nyab xeeb thiab dav qhia. Nrog cov txheej txheem optimization thiab cov kev txhim kho tshiab ntawm kev txhim kho daim foos, nws lub peev xwm hauv kev kho tus kheej thiab kev sib xyaw yuav raug tso tawm ntxiv. Nyob rau hauv lub neej yav tom ntej, hauv-tob kev tshawb fawb tsis zoo cov txheej txheem yuav txhawb nqa lub sijhawm ntev ntawm cov kev kho mob qog.