Inxight Drugs

Search results for "EMA EPAR|DISEASES|BLOOD AND LYMPHATIC DISEASES|HEMATOLOGIC DISEASES" in comments (approximate match)

Showing 1 - 10 of 24 results

DEFERIPRONE

MORE DETAILS

2BTY8KH53L

Status:

US Approved Rx (2020)

First approved in 2011

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Deferiprone (trade name Ferriprox) is an iron chelator indicated for the treatment of patients with transfusional iron overload due to thalassemia syndromes when current chelation therapy is inadequate. Deferiprone is an orally bioavailable bidentate...

PLERIXAFOR

MORE DETAILS

S915P5499N

Status:

US Approved Rx (2023)

First approved in 2008

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Plerixafor is a bicyclam molecule, which has been identified as a specific antagonist of CXCR4. It had originally been developed as an inhibitor of T-tropic human immunodeficiency virus, but later demonstrated to be an effective mobilizer of hematop...

DEFERASIROX

MORE DETAILS

V8G4MOF2V9

Status:

US Approved Rx (2022)

First approved in 2005

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Deferasirox (marketed as Exjade, Desirox, Deferasirox) is an iron chelator. Its main use is to reduce chronic iron overload in patients who are receiving long term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. ...

LENALIDOMIDE

MORE DETAILS

F0P408N6V4

Status:

US Approved Rx (2021)

First approved in 2005

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Conditions:

Lenalidomide (trade name Revlimid) is a derivative of thalidomide introduced in 2004. It is an immunomodulatory agent with anti-angiogenic properties. Revlimid in combination with dexamethasone is indicated for the treatment of patients with multipl...

e myeloma (MM) who have received at least one prior therapy. Also is indicated for the treatment of patients with transfusion-dependent anemia due to low- or intermediate-1-risk myelodysplastic syndromes (MDS) associated with a deletion 5q cytogenetic abnormality with or without additional cytogenetic abnormalities. In addition, Revlimid is indicated for the treatment of patients with mantle cell lymphoma (MCL) whose disease has relapsed or progressed after two prior therapies, one of which included bortezomib. The mechanism of action of lenalidomide remains to be fully characterized. Lenalidomide inhibited the secretion of pro-inflammatory cytokines and increased the secretion of anti-inflammatory cytokines from peripheral blood mononuclear cells. Lenalidomide causes a delay in tumor growth in some in vivo nonclinical hematopoietic tumor models including multiple myeloma. Immunomodulatory properties of lenalidomide include activation of T cells and natural killer (NK) cells, increased numbers of NKT cells, and inhibition of pro-inflammatory cytokines (e.g., TNF-α and IL-6) by monocytes. In multiple myeloma cells, the combination of lenalidomide and dexamethasone synergizes the inhibition of cell proliferation and the induction of apoptosis. Recently was discovered, that protein cereblon (CRBN) is a proximate, therapeutically important molecular target of lenalidomide. Low CRBN expression was found to correlate with drug resistance in multiple myeloma (MM) cell lines and primary MM cells. One of the downstream targets of CRBN identified is interferon regulatory factor 4 (IRF4), which is critical for myeloma cell survival and is down-regulated by (immune-modulatory drugs) treatment. CRBN is also implicated in several effects of immunomodulatory drugs, such as down-regulation of tumor necrosis factor-α (TNF-α) and T cell immunomodulatory activity, demonstrating that the pleotropic actions of the immunomodulatory drugs (IMiDs) are initiated by binding to CRBN. Future dissection of CRBN downstream signaling will help to delineate the underlying mechanisms for IMiD action and eventually lead to development of new drugs with more specific anti-myeloma activities. It may also provide a biomarker to predict IMiD response and resistance. Lenalidomide also inhibited the expression of cyclooxygenase-2 (COX-2) but not COX-1 in vitro.

BORTEZOMIB

MORE DETAILS

69G8BD63PP

Status:

US Approved Rx (2022)

First approved in 2003

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Bortezomib is the therapeutic proteasome inhibitor. First, which is tested in humans. The boron atom in bortezomib binds the catalytic site of the 26S proteasome with high affinity and specificity. Bortezomib is approved in the U.S. for treating rela...

THALIDOMIDE

MORE DETAILS

4Z8R6ORS6L

Status:

US Approved Rx (1998)

First approved in 1998

Class (Stereo):

CHEMICAL (RACEMIC)

Targets:

Conditions:

Thalidomide is an immunomodulatory agent with a spectrum of activity that is not fully characterized. Thalidomide is racemic — it contains both left and right-handed isomers in equal amounts: one enantiomer is effective against morning sickness, and ...

Hydroxyurea

MORE DETAILS

X6Q56QN5QC

Status:

US Approved Rx (1998)

First approved in 1967

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Conditions:

Hydroxyurea is an oral antimetabolite; inhibits ribonucleotide reductase and DNA synthesis. It is used for resistant chronic myeloid leukemia, locally advanced squamous cell carcinomas of the head and neck (excluding lip) in combination with concurre...