Orale Wirkstoffe A

Abemaciclib – VERZENIOS®

According to the NCI website Abemaciclib is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. Abemaciclib specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. 

Indikationen gemäss Compendium.ch®

Verzenios ist angezeigt zur Behandlung von postmenopausalen Frauen mit Hormonrezeptor (HR)-positivem, humanem epidermalen Wachstumsfaktor-Rezeptor-2 (HER2)-negativem lokal fortgeschrittenem oder metastasiertem Brustkrebs:

  • in Kombination mit einem Aromatasehemmer als initiale endokrine Therapie;
  • in Kombination mit Fulvestrant bei Frauen, nach vorheriger endokriner Therapie;
  • als Monotherapie nach Progression der Erkrankung nach endokriner Therapie und einem oder zwei Chemotherapie-Regimen bei metastasierter Erkrankung, wenn eine Chemotherapie nicht geeignet ist.

Link zur Fachinformation von Compendium.ch®:

Medikamenteniformation: Für den Arzt 

More Information in English:

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health

Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu Wiki

Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Info for Patients presented by Scott Hamilton from Chemocare.com

 

Abirateron - ZYTIGA®

Zytiga®  ist ein oral verfügbares Azetat-Salz des antiandrogenen Steroids Abirateron. Es hemmt die enzymatische Aktivität der Steroid-17alpha-Monooxygenase (17alpha-hydrolase/C17,20 Lyase Komplex), einem Mitglied der Zytochrom p450 Familie. Dieses katalysiert die 17alpha-Hydroxylierung der Steroid-Zwischenprodukte, die an der Testosteron  Synthese beteiligt sind. Die Verabreichung des Wirkstoffes kann die Bildung von Testosteron sowohl in den Hoden als auch in den Nebennieren bis auf ein Kastrationsniveau unterdrücken.  

 

Indikationen/Anwendungsmöglichkeiten gemäss Compendium®:

  • Zur Behandlung in Kombination mit LHRH Agonisten und Prednison oder Prednisolon bei Patienten mit fortgeschrittenem metastasierenden Prostatakarzinom bei Progredienz nach Behandlung mit Docetaxel.
  • Zur Behandlung in Kombination mit LHRH Agonisten und Prednison oder Prednisolon bei asymptomatischen oder leicht symptomatischen Patienten mit metastasierendem, kastrationsresistentem Prostatakarzinom (mCRPC) ohne viszerale Metastasen und ohne Lebermetastasen, nach Versagen der Androgendeprivationstherapie, wenn eine Chemotherapie klinisch nicht indiziert ist.
  • Zur Behandlung in Kombination mit Prednison oder Prednisolon und Androgendeprivationstherapie (ADT) bei Patienten mit neu diagnostiziertem Hochrisiko-metastasiertem hormonsensitivem Prostatakarzinom (mHSPC) (siehe «Klinische Wirksamkeit»).
 
 
 
Link zur Fachinformation des Compendium®:
 
Medikamenteniformation: 
Information des Médicaments:
 
Informazione sul medicamento: 

Merkblatt für Patientinnen und Patienten

More Information in English:

Link to National Cancer Institute
Link zu Wiki
Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)

 

 
Acalabrutinib – CALQUENCE® (USA)

According to the NCI website Acalabrutinib orally available inhibitor of Bruton’s tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, acalabrutinib inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. 

Indicated according to Chemocare for: 

  • The treatment of adult patients with mantle cell lymphoma (MCL) who have received at least one prior therapy.
  • The treatment of adult patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL).

More Information in English:

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health

Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu Wiki

Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Info for Patients presented by Scott Hamilton from Chemocare.com

Afatinib - GIOTRIF®

Afatinib ist ein oral verfügbarer dualer Tyrosin-Kinase-Rezeptor (RTK) Inhibitor mit einer potentiell antineoplastischen Aktivität. Afatinib bindet sich irreversibel an die humanen epidermalen Wachstumsfaktoren 1 und 2 (EGFR-1; HER2) und hemmt sie auch irreversibel. Dies kann zu einer Hemmung des Tumorwachstums sowie der Gefässneubildung (Angiogenese) führen. EGFR/HER2 sind RTKs, die zur EGFR Superfamilie gehören. Beide spielen eine bedeutende Rolle bei der Proliferation der Tumorzellen und bei der Gefässversorgung des Tumors und werden in vielen Krebszellen überexprimiert.

 

Indikationen/Anwendungsmöglichkeiten gemäss Compendium®:

  • Giotrif ist als Monotherapie für Patienten mit nicht-kleinzelligem Lungenkarzinom (NSCLC, Stadium IIIb/IV) mit aktivierenden Mutationen des EGFR (Exon 19 Deletionen, Exon 18 G719X Substitutionen, Exon 20 S768I Substitutionen sowie Exon 21 L858R Substitutionen und L861Q Substitutionen) indiziert, die nicht mit EGFR-TKIs vorbehandelt sind.
  • Giotrif ist zur Behandlung von Patienten mit einem lokal fortgeschrittenen oder metastasierten Plattenepithelkarzinom der Lunge indiziert, deren Karzinom während oder nach einer platinhaltigen Chemotherapie fortgeschritten ist und die für eine Immuntherapie nicht geeignet sind.

Merkblätter für Patientinnen und Patienten

Link zur Fachinformation des Compendium®:

Medikamenteniformation: Für den Arzt  Patienteninformation

Information des Médicaments: Info prof.  Info patient

Informazione sul medicamento: info per il paziente

 

More Information in English

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu Wiki

Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Info for Patients presented by Scott Hamilton from Chemocare.com

Receptor tyrosine kinases (RTK)s are very important signaling pathway, which not only include growth factor receptors such as EGFR(HER)VEGFR PDGFRFGGFRIGF-1R, Mast/stem cell growth factor receptor ( c-Met) and HER2, but also other gene products which are expressed by the oncogenes such as SRC, Bcr, c-Met and Abl as well. Read more at selleckbio about Receptor Tyrosine Kinase Signaling Pathway

Tyrosin Kinase Inhibitor

Alectinib - ALECENSA®

According to the NCI website Alectinib is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity. Upon administration, alectinib binds to and inhibits ALK kinase, ALK fusion proteins as well as the gatekeeper mutation ALKL1196M known as one of the mechanisms of acquired resistance to small-molecule kinase inhibitors. The inhibition leads to disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-overexpressing tumor cells. 

Indikationen/Anwendungsmöglichkeiten gemäss Compendium®
  • Alecensa ist für die Behandlung von Patienten mit lokal fortgeschrittenem oder metastasiertem ALK (Anaplastic-lymphoma-kinase)-positivem nicht-kleinzelligem Lungenkarzinom (NSCLC) indiziert.

Medikamenteniformation:

 
 
More info for patients:

ALK-Inhibitors

 

Alitretinoin
 
Toctino®; According to the NCI website alitretinoin is an orally- and topically-active naturally-occurring retinoic acid with antineoplastic, chemopreventive, teratogenic, and embryotoxic activities. Alitretinoin binds to and activates nuclear retinoic acid receptors (RAR) and retinoid X receptors (RXR); these activated receptors act as transcription factors, regulating gene expression that results in the inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells.


(According to MedlinePlus Alitretinoin is used to treat skin lesions associated with Kaposi's sarcoma. It helps stop the growth of Kaposi's sarcoma cells.
This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.)
Toctino ist indiziert bei Erwachsenen mit therapierefraktärem, schwerem chronischem Handekzem, die eine ausgebaute lokale Behandlung für mindestens 4 Wochen erhalten und nicht darauf angesprochen haben. Die Vorbehandlung schliesst die Vermeidung von Kontakten mit der auslösenden Noxe, Hautschutz und potente topische ­Kortikosteroide ein.

Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu Wiki
Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Link zur Fachinformation des Compendium®
Info for Patients presented by Scott Hamilton from Chemocare.com
Chemotherapy
Alpelisib - PIQRAY®
According to the NCI website Alpelisib is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. Alpelisib specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. 

Indikation gemäss Compendium®

  • Piqray wird in Kombination mit Fulvestrant angewendet für die Behandlung von postmenopausalen Frauen mit Hormon-Rezeptor (HR)-positivem, humanen epidermalen Wachstumsfaktor-Rezeptor-2 (HER2)-negativem fortgeschrittenem Brustkrebs mit einer PIK3CA-Mutation nach Fortschreiten der Erkrankung, wenn die Patienten zuvor eine endokrine Therapie einschliesslich eines Aromatase Inhibitors erhalten haben.

Arzneimittelinformation gemäss Compendium®

More Information in English:

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health

Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu Wiki

Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Info for Patients presented by Scott Hamilton from Chemocare.com

AMG-510/Sotorasib

According to the NCI website, KRAS mutant-targeting AMG 510 (sotorasib ) is an orally available agent that targets the specific KRAS mutation, p.G12C, with potential antineoplastic activity. Upon oral administration, KRAS mutant-targeting AMG 510 selectively targets the KRAS p.G12C mutant, at either the DNA, RNA or protein level, and prevents, through an as of yet not elucidated manner, expression of and/or tumor cell signaling through the KRAS p.G12C mutant. This may inhibit growth in KRAS p.G12C-expressing tumor cells. The KRAS p.G12C mutation is seen in some tumor cell types and plays a key role in tumor cell proliferation. Check for active clinical trials using this agent. (NCI Thesaurus)

More Information in English:

Inxight: Drugs (NIH)

AdisInsight

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute

Wiki

Amuvatinib

According to the NCI website, amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity. Amuvatinib binds to mutant forms of the stem cell factor receptor (c-Kit; SCFR), inhibiting clinically relevant mutants of this receptor tyrosine kinase that may be associated with resistance to therapy. In addition, amuvatinib inhibits activities of other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFR alpha, which are frequently dysregulated in variety of tumors. This agent also suppresses the induction of DNA repair protein Rad51, thereby potentiating the activities of DNA damage-inducing agents. Mutant forms of c-Kit are often associated with tumor chemoresistance. 

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute

According the Website of SELLECKBIO Amuvatinib (MP-470) is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM. MP-470(MP 470, MP470) reduced c-Met phosphorylation and enhanced radiation-induced cell kill by 0.4 logs in SF767 cells. Cells pretreated with MP-470 had more ds DNA damage than cells treated with radiation alone. Mechanistically, MP-470 was shown to inhibit dsDNA break repair and increase apoptosis. [1][2] In a study, the cytotoxicity of MP-470 was evaluated on prostate cancer cell lines (LNCaP, PC-3 and DU-145). MP-470(MP 470, MP470) was effective on LNCaP and PC-3 cells with IC50 of ~4 μM and 8 μM, respectively. [3]


Receptor tyrosine kinases (RTK)s are very important signaling pathway, which not only include growth factor receptors such as EGFR(HER)VEGFR PDGFRFGGFRIGF-1R, Mast/stem cell growth factor receptor ( c-Met) and HER2, but also other gene products which are expressed by the oncogenes such as SRC, Bcr, c-Met and Abl as well. Read more at selleckbio about Receptor Tyrosine Kinase Signaling Pathway

Tyrosin Kinase Inhibitor

Anagrelide - XAGRID®, THROMBOREDUCTIN® ANAGRELID NORDIC®

According to the NCI website, anagrelide hydrochloride is the salt of a synthetic quinazoline derivative; anagrelide hydrochloride reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis. Check for active clinical trials using this agent. (NCI Thesaurus)



Indikationen/Anwendungsmöglichkeiten gemäss Compendium®:

XAGRID®: Merkblätter für Patientinnen und Patienten


Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health

Link to National Cancer Institute

Link zu Wiki
Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Info for Patients presented by Scott Hamilton from Chemocare.com

Anastrozol - ARIMIDEX® und diverse Generika
Arimidex® sowie diverse Generika - A nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure.

Indikationen/Anwendungsmöglichkeiten gemäss Compendium®:
  • Adjuvante Behandlung beim Mammakarzinom mit Östrogen- oder Progesteron-Rezeptor-positivem oder mit unbekanntem Hormon-Rezeptor-Status (Stadium I und II) bei postmenopausalen Frauen.
  • Behandlung des fortgeschrittenen Mammakarzinoms bei postmenopausalen Frauen.
 

 

Link zur Fachinformation des Compendium®:

Medikamenteniformation: Für den Arzt  Patienteninformation

Information des Médicaments: Info prof.  Info patient

Informazione sul medicamento: info per il paziente


Link to National Cancer Institute
Link to Wikipedia
Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Info for Patients presented by Scott Hamilton from Chemocare.com
Apalutamide - ERLEADA®

According to the NCI website, Apalutamide is a  small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity. Apalutamide binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells. Check for active clinical trials using this agent. (NCI ThesaurusPatient Information

Indikationen/Anwendungsmöglichkeiten gemäss Compendium®

  • ERLEADA in Kombination mit einer Androgendeprivationstherapie (ADT) ist indiziert für die Behandlung von erwachsenen Patienten mit nicht-metastasiertem, kastrationsresistentem Prostatakarzinom (NM-CRPC), bei denen ein hohes Risiko für eine Entwicklung von Metastasen besteht (insbesondere PSADT ≤10 Monate; siehe «Klinische Wirksamkeit»).

 

Link zur Fachinformation von Compendium.ch®

Link zur Patienteninfo von Compndium®

Merkblätter für Patientinnen und Patienten (am 16.6.20 noch nicht erhältlich gewesen)

 

More Information in English:

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health

Link to MedlinePlus, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute

Wiki

Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)

Info for Patients presented by Scott Hamilton from Chemocare.com

Apatinib / Rivoceranib

 

According to the NCI website, apatinib is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases. Check for active clinical trials using this agent. (NCI Thesaurus)

 

More Information in English:

Inxight: Drugs (NIH)

AdisInsight

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute

Wiki
Link to European Medicines Agency (EMEA)

ARV-110 - androgen receptor degrader

According to the NCI website, ARV-110 is an orally available selective androgen receptor (AR)-targeted protein degrader, using the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic activity. ARV-110 is composed of an AR ligand attached to an E3 ligase recognition moiety. Upon oral administration, ARV-110 targets and binds to the AR ligand binding domain. E3 ligase is recruited to the AR by the E3 ligase recognition moiety and the AR target protein is tagged by ubiquitin. This causes ubiquitination and degradation of AR by the proteasome. This prevents the expression of AR target genes and halts AR-mediated signaling. This results in an inhibition of proliferation in AR-overexpressing tumor cells. In addition, the degradation of the AR protein releases the ARV-110 is released and can bind to additional AR target proteins. AR plays a key role in the proliferation of castration-resistant prostate cancer cells (CRPC). Check for active clinical trials using this agent. (NCI Thesaurus)


Link to National Cancer Institute

Asciminib

According to the NCI website, Asciminib is An orally bioavailable, allosteric Bcr-Abl tyrosine kinase inhibitor with potential antineoplastic activity. Designed to overcome resistance, asciminib binds to the Abl portion of the Bcr-Abl fusion protein at a location that is distinct from the ATP-binding domain. This binding results in the inhibition of Bcr-Abl-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies. The Bcr-Abl fusion protein tyrosine kinase is an abnormal enzyme produced by leukemia cells that contain the Philadelphia chromosome. Check for active clinical trials using this agent. (NCI Thesaurus)

 

More Information in English:

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link to European Medicines Agency (EMEA)

 

Avadomide

According to the NCI website, Avadomide is a  novel, small molecule cereblon-modulating agent with potential antineoplastic, antiangiogenic and immunomodulatory activities. Upon oral administration, avadomide binds to and modulates cereblon to promote recruitment of the hematopoietic transcription factors Aiolos and Ikaros to the Cullin-4 RING E3 ubiquitin ligase complex. This binding results in the ubiquitination and rapid proteasomal degradation of Aiolos and Ikaros and the derepression of interferon (IFN)-stimulated genes, including DDX58 and IRF7, leading to apoptosis of certain tumor cells. Additionally, Aiolos degredation leads to derepression of the IL2 gene, thereby enhancing interleukin-2 production, costimulation of T lymphocytes and IL-2-induced T-cell proliferation. Avadomide may also promote the activation of natural killer (NK) cells, potentially enhancing tumor cell killing. Aiolos and Ikaros are transcriptional repressors known to play an important role in normal B and T cell function. Check for active clinical trials using this agent. (NCI Thesaurus)

 

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link to European Medicines Agency (EMEA)

 

Axitinib - INLYTA®

Axitinib ist ein oral verfügbarer Tyrosin Kinase Hemmer. Er hemmt den Rezeptor für den vaskulären endothelialen Wachstumsfaktor (VEGF), ein gefässbildungsförderndes Zytokin sowie den Rezeptor für den von Blutplättchen freigesetzten Wachstumsfaktor (PDGF). Dies führt zu einer Hemmung der Blutgefässbildung.  

Indikationen/Anwendungsmöglichkeiten gemäss Compendiums®:

Inlyta® ist indiziert zur Behandlung von Patienten mit fortgeschrittenem Nierenzellkarzinom (RCC) nach Versagen einer vorherigen systemischen Therapie.

Merkblätter für Patientinnen und Patienten

Link zur Fachinformation des Compendiums®:
Medikamenteniformation: Für den Arzt  Patienteninformation
Information des Médicaments: Info prof.  Info patient
Informazione sul medicamento: info per il paziente

 

More Information in English:

Link to Drug Information Portal, a service of the U.S. National Library of Medicine, National Institutes of Health
Link to National Cancer Institute
Link zu Wiki

Link zu PharmaWiki
Link to Physicians Desk Reference (PDR)
Link to European Medicines Agency (EMEA)
Info for Patients presented by Scott Hamilton from Chemocare.com


Tyrosin Kinase Inhibitor