Peringatan Keamanan

The reported oral Ld50 is of 100 mg/kg.MSDS In cases of overdosage, only supportive measures are considered.FDA label

Palbociclib was showed to present clastogenic activities in in vitro and in vivo assays. As well, it has been reported to produce fetal harm due to its mechanism of action.A176792 Lastly, it was shown to increase the incidence of microglial cell tumors in the central nervous system at high doses.FDA label

Palbociclib

DB09073

small molecule approved investigational

Deskripsi

Palbociclib is a piperazine pyridopyrimidineA176792 that acts in the cell cycle machinery. It is a second generation cyclin-dependent kinase inhibitorA176798 selected from a group of pyridopyrimidine compounds due to its favorable physical and pharmaceutical properties.A176810

Palbociclib was developed by Pfizer Inc after the discovery that identified the cyclin-dependent kinases as key regulators of cell growth.L5867 It was originally FDA approved on March 2015 for the treatment of HR-positive, HER2-negative advanced or metastatic breast cancer and its indications were updated in April 2019 to include male patients based on findings from postmarketing reports and electronic health records demonstrating safety and clinical efficacy.L4894

Struktur Molekul 2D

Berat 447.5328
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean plasma elimination half-life of palbociclib is 29 hours.[A176792]
Volume Distribusi The mean apparent distribution of palbociclib is 2583 L which suggests that palbociclib penetrates extensively into peripheral tissues.[L5876]
Klirens (Clearance) The mean apparent oral clearance of palbociclib is of 63.1 L/h.[A176792]

Absorpsi

Palbociclib presents a linear pharmacokinetic profile and its peak plasma concentration was observed 6-12 hours after oral administration. The oral bioavailability is reported to be of 46% with a steady-state reached after 8 days and a median accumulation ratio of 2.4.A176792 The absorption of palbociclib is significantly reduced under fasting conditions and hence, food intake is recommended when this drug is administered.A176792

Metabolisme

Palbociclib is mainly hepatically transformed.A176792 the metabolism is mainly performed by the activities of the cytochrome P450 isoenzyme 3A and the sulfotransferase 2A1.A176798 The metabolism of palbociclib is represented mainly by reactions of oxidation and sulfonation followed by acylation and glucuronidation as minor reactions. After its metabolism, palbociclib forms mainly inactive glucuronide and sulfamic acid conjugates. The major circulating metabolite, accounting for 1.5% of the dose in excreta is is the glucuronide conjugate.F4265

Rute Eliminasi

The main route of elimination of palbociclib is through feces after hepatic metabolism while renal clearance seems to play a minor role accounting only for 17.5% of the eliminated dose.A176792

Interaksi Makanan

5 Data
  • 1. Avoid grapefruit products. Grapefruit inhibits the CYP3A metabolism of palbociclib, which may increase its serum concentration.
  • 2. Avoid St. John's Wort. This herb induces the CYP3A metabolism of palbociclib and may reduce its serum concentration.
  • 3. Take at the same time every day. This applies to both palbociclib capsules and tablets.
  • 4. Take with food. Palbociclib capsules should be taken with food. Some subjects have reduced bioavailability of palbociclib when in a fasted state, therefore taking with food makes the bioavailability more consistent.
  • 5. Take with or without food. Palbociclib tablets may be taken with or without food.

Interaksi Obat

1114 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Palbociclib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Palbociclib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Palbociclib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Palbociclib.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Palbociclib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Palbociclib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Palbociclib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Palbociclib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Palbociclib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Palbociclib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Palbociclib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Palbociclib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Palbociclib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Palbociclib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Palbociclib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Palbociclib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Palbociclib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Palbociclib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Palbociclib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Palbociclib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Palbociclib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Palbociclib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Palbociclib.
Cladribine The excretion of Cladribine can be decreased when combined with Palbociclib.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Palbociclib.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Palbociclib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Palbociclib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Palbociclib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Palbociclib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Palbociclib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Palbociclib.
Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Palbociclib.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Palbociclib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Palbociclib.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Palbociclib.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Palbociclib.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Palbociclib.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Palbociclib.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Palbociclib.
Zidovudine The risk or severity of adverse effects can be increased when Zidovudine is combined with Palbociclib.
Cisplatin The risk or severity of adverse effects can be increased when Cisplatin is combined with Palbociclib.
Oxaliplatin The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Palbociclib.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Palbociclib.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Palbociclib.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Palbociclib.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Palbociclib.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Palbociclib.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Palbociclib.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Palbociclib.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Palbociclib.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Palbociclib.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Palbociclib.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Palbociclib.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Palbociclib.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Palbociclib.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Palbociclib.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Palbociclib.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Palbociclib.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Palbociclib.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Palbociclib.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Palbociclib.
Mercaptopurine The risk or severity of adverse effects can be increased when Mercaptopurine is combined with Palbociclib.
Thalidomide The metabolism of Palbociclib can be increased when combined with Thalidomide.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Palbociclib.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Palbociclib.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Palbociclib.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Palbociclib.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Palbociclib.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Palbociclib.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Palbociclib.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Palbociclib.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Palbociclib.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Palbociclib.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Palbociclib.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Palbociclib.
Ciclesonide The risk or severity of adverse effects can be increased when Ciclesonide is combined with Palbociclib.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Palbociclib.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Palbociclib.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Palbociclib.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Palbociclib.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Palbociclib.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Palbociclib.
Aldosterone The risk or severity of adverse effects can be increased when Aldosterone is combined with Palbociclib.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Palbociclib.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Palbociclib.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Palbociclib.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Palbociclib.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Palbociclib.
Mepolizumab The risk or severity of adverse effects can be increased when Mepolizumab is combined with Palbociclib.
Abetimus The risk or severity of adverse effects can be increased when Abetimus is combined with Palbociclib.
Belatacept The risk or severity of adverse effects can be increased when Belatacept is combined with Palbociclib.
Pralatrexate The risk or severity of adverse effects can be increased when Pralatrexate is combined with Palbociclib.
Wortmannin The risk or severity of adverse effects can be increased when Wortmannin is combined with Palbociclib.
Eribulin The risk or severity of adverse effects can be increased when Eribulin is combined with Palbociclib.
Belimumab The risk or severity of adverse effects can be increased when Belimumab is combined with Palbociclib.
Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Palbociclib.
Dimethyl fumarate The risk or severity of adverse effects can be increased when Dimethyl fumarate is combined with Palbociclib.
Obinutuzumab The risk or severity of adverse effects can be increased when Obinutuzumab is combined with Palbociclib.
Vedolizumab The risk or severity of adverse effects can be increased when Vedolizumab is combined with Palbociclib.
Blinatumomab The risk or severity of adverse effects can be increased when Blinatumomab is combined with Palbociclib.

Target Protein

Cyclin-dependent kinase 4 CDK4
Cyclin-dependent kinase 6 CDK6

Referensi & Sumber

Artikel (PubMed)
  • PMID: 28752187
    Wilson FR, Varu A, Mitra D, Cameron C, Iyer S: Systematic review and network meta-analysis comparing palbociclib with chemotherapy agents for the treatment of postmenopausal women with HR-positive and HER2-negative advanced/metastatic breast cancer. Breast Cancer Res Treat. 2017 Nov;166(1):167-177. doi: 10.1007/s10549-017-4404-4. Epub 2017 Jul 27.
  • PMID: 28680952
    Nathan MR, Schmid P: A Review of Fulvestrant in Breast Cancer. Oncol Ther. 2017;5(1):17-29. doi: 10.1007/s40487-017-0046-2. Epub 2017 May 8.
  • PMID: 26324739
    Beaver JA, Amiri-Kordestani L, Charlab R, Chen W, Palmby T, Tilley A, Zirkelbach JF, Yu J, Liu Q, Zhao L, Crich J, Chen XH, Hughes M, Bloomquist E, Tang S, Sridhara R, Kluetz PG, Kim G, Ibrahim A, Pazdur R, Cortazar P: FDA Approval: Palbociclib for the Treatment of Postmenopausal Patients with Estrogen Receptor-Positive, HER2-Negative Metastatic Breast Cancer. Clin Cancer Res. 2015 Nov 1;21(21):4760-6. doi: 10.1158/1078-0432.CCR-15-1185. Epub 2015 Aug 31.
  • PMID: 28203301
    Rocca A, Schirone A, Maltoni R, Bravaccini S, Cecconetto L, Farolfi A, Bronte G, Andreis D: Progress with palbociclib in breast cancer: latest evidence and clinical considerations. Ther Adv Med Oncol. 2017 Feb;9(2):83-105. doi: 10.1177/1758834016677961. Epub 2016 Nov 21.
  • PMID: 25177151
    Cadoo KA, Gucalp A, Traina TA: Palbociclib: an evidence-based review of its potential in the treatment of breast cancer. Breast Cancer (Dove Med Press). 2014 Aug 4;6:123-33. doi: 10.2147/BCTT.S46725. eCollection 2014.
  • PMID: 27493617
    Schmidt M: Palbociclib - from Bench to Bedside and Beyond. Breast Care (Basel). 2016 Jun;11(3):177-81. doi: 10.1159/000447001. Epub 2016 Jun 22.

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