Synthesis and Clinical Development of Palbociclib : An Overview
Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net..
Breast cancer is the second most commonly identified cancer in women in the United States after skin cancer. The past few years have seen a substantial increase in breast cancer awareness campaigns and active research in fields of diagnosis and targeted therapy. These factors have led to a better mechanistic understanding of the disease, detection at earlier stages, and a more personalized approach to treatment, ultimately causing a crucial increase in the survival rates after detection. However, with the advances in treatment, cases of patients developing primary resistance and acquired resistance are increasing. Most of the breast cancers which develop resistance to therapy are ER+ and are typically treated with tamoxifen and fulvestrant. These drugs either lower the levels of estrogen or inhibit the receptors for estrogen and prevent the tumor from spreading. Around one-third of women treated with these drugs develop resistance to them, lowering their chances of survival. This has directed the search for newer drug therapies to target advanced breast cancer and resistance. One of these efforts has resulted in the development of Palbociclib, a first in class inhibitor of cyclin dependent kinases 4 and 6 (CDK4 and CDK6), which was granted accelerated approval from the FDA for combination therapy in postmenopausal women with ER+, HER2- metastatic breast cancer. This review is focused on the various aspects of "Palbociclib" including its synthesis, molecular modeling studies, and efficacy and safety profile with data obtained from various clinical trials.
| Medienart: |
E-Artikel |
|---|
| Erscheinungsjahr: |
2022 |
|---|---|
| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:18 |
|---|---|
| Enthalten in: |
Medicinal chemistry (Shariqah (United Arab Emirates)) - 18(2022), 1 vom: 25., Seite 2-25 |
| Sprache: |
Englisch |
|---|
| Beteiligte Personen: |
Konar, Debabrata [VerfasserIn] |
|---|
| Links: |
|---|
| Themen: |
Breast cancer |
|---|
| Anmerkungen: |
Date Completed 19.01.2022 Date Revised 19.01.2022 published: Print Citation Status MEDLINE |
|---|
| doi: |
10.2174/1573406417666201204161243 |
|---|
| funding: |
|
|---|---|
| Förderinstitution / Projekttitel: |
|
| PPN (Katalog-ID): |
NLM318464861 |
|---|
| LEADER | 01000naa a22002652 4500 | ||
|---|---|---|---|
| 001 | NLM318464861 | ||
| 003 | DE-627 | ||
| 005 | 20231225165417.0 | ||
| 007 | cr uuu---uuuuu | ||
| 008 | 231225s2022 xx |||||o 00| ||eng c | ||
| 024 | 7 | |a 10.2174/1573406417666201204161243 |2 doi | |
| 028 | 5 | 2 | |a pubmed24n1061.xml |
| 035 | |a (DE-627)NLM318464861 | ||
| 035 | |a (NLM)33280599 | ||
| 040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
| 041 | |a eng | ||
| 100 | 1 | |a Konar, Debabrata |e verfasserin |4 aut | |
| 245 | 1 | 0 | |a Synthesis and Clinical Development of Palbociclib |b An Overview |
| 264 | 1 | |c 2022 | |
| 336 | |a Text |b txt |2 rdacontent | ||
| 337 | |a ƒaComputermedien |b c |2 rdamedia | ||
| 338 | |a ƒa Online-Ressource |b cr |2 rdacarrier | ||
| 500 | |a Date Completed 19.01.2022 | ||
| 500 | |a Date Revised 19.01.2022 | ||
| 500 | |a published: Print | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright© Bentham Science Publishers; For any queries, please email at epubbenthamscience.net. | ||
| 520 | |a Breast cancer is the second most commonly identified cancer in women in the United States after skin cancer. The past few years have seen a substantial increase in breast cancer awareness campaigns and active research in fields of diagnosis and targeted therapy. These factors have led to a better mechanistic understanding of the disease, detection at earlier stages, and a more personalized approach to treatment, ultimately causing a crucial increase in the survival rates after detection. However, with the advances in treatment, cases of patients developing primary resistance and acquired resistance are increasing. Most of the breast cancers which develop resistance to therapy are ER+ and are typically treated with tamoxifen and fulvestrant. These drugs either lower the levels of estrogen or inhibit the receptors for estrogen and prevent the tumor from spreading. Around one-third of women treated with these drugs develop resistance to them, lowering their chances of survival. This has directed the search for newer drug therapies to target advanced breast cancer and resistance. One of these efforts has resulted in the development of Palbociclib, a first in class inhibitor of cyclin dependent kinases 4 and 6 (CDK4 and CDK6), which was granted accelerated approval from the FDA for combination therapy in postmenopausal women with ER+, HER2- metastatic breast cancer. This review is focused on the various aspects of "Palbociclib" including its synthesis, molecular modeling studies, and efficacy and safety profile with data obtained from various clinical trials | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Review | |
| 650 | 4 | |a Breast cancer | |
| 650 | 4 | |a CDK4 | |
| 650 | 4 | |a CDK6 | |
| 650 | 4 | |a Clinical trial | |
| 650 | 4 | |a Palbociclib | |
| 650 | 4 | |a carcinoma. | |
| 650 | 7 | |a Piperazines |2 NLM | |
| 650 | 7 | |a Protein Kinase Inhibitors |2 NLM | |
| 650 | 7 | |a Pyridines |2 NLM | |
| 650 | 7 | |a Receptors, Estrogen |2 NLM | |
| 650 | 7 | |a Receptor, ErbB-2 |2 NLM | |
| 650 | 7 | |a EC 2.7.10.1 |2 NLM | |
| 650 | 7 | |a palbociclib |2 NLM | |
| 650 | 7 | |a G9ZF61LE7G |2 NLM | |
| 700 | 1 | |a Maru, Saurabh |e verfasserin |4 aut | |
| 700 | 1 | |a Kar, Subhabrata |e verfasserin |4 aut | |
| 700 | 1 | |a Kumar, Kapil |e verfasserin |4 aut | |
| 773 | 0 | 8 | |i Enthalten in |t Medicinal chemistry (Shariqah (United Arab Emirates)) |d 2005 |g 18(2022), 1 vom: 25., Seite 2-25 |w (DE-627)NLM163628467 |x 1875-6638 |7 nnns |
| 773 | 1 | 8 | |g volume:18 |g year:2022 |g number:1 |g day:25 |g pages:2-25 |
| 856 | 4 | 0 | |u http://dx.doi.org/10.2174/1573406417666201204161243 |3 Volltext |
| 912 | |a GBV_USEFLAG_A | ||
| 912 | |a GBV_NLM | ||
| 951 | |a AR | ||
| 952 | |d 18 |j 2022 |e 1 |b 25 |h 2-25 | ||