Definition
ChEBI: Plerixafor is an azamacrocycle consisting of two cyclam rings connected by a 1,4-phenylenebis(methylene) linker. It is a CXCR4 chemokine receptor antagonist and a hematopoietic stem cell mobilizer. It is used in combination with grulocyte-colony stimulating factor (G-CSF) to mobilize hematopoietic stem cells to the perpheral blood for collection and subsequent autologous transplantation in patients with non-Hodgkin's lymphoma and multiple myeloma. It has a role as an immunological adjuvant, an antineoplastic agent, an anti-HIV agent and a C-X-C chemokine receptor type 4 antagonist. It is an azamacrocycle, a crown amine, a secondary amino compound, an azacycloalkane, a tertiary amino compound and a member of benzenes. It is functionally related to a 1,4,8,11-tetraazacyclotetradecane.
Side effects
The most common adverse reactions (occurring in more than 10% of patients) observed during plerixafor use include diarrhea, nausea, fatigue, injection-site reactions, headache, arthralgia, dizziness, and vomiting.
References
[1]zabel ba, wang y, lewén s, berahovich rd, penfold me, zhang p, powers j, summers bc, miao z, zhao b, jalili a, janowska-wieczorek a, jaen jc, schall tj. elucidation of cxcr7-mediated signaling events and inhibition of cxcr4-mediated tumor cell transendothelial migration by cxcr7 ligands. j immunol. 2009 sep 1;183(5):3204-11.
[2].li j, oupicky d. effect of biodegradability on cxcr4 antagonism, transfection efficacy and antimetastatic activity of polymeric plerixafor.biomaterials. 2014 jul;35(21):5572-9.
[3]. broxmeyer he. chemokines in hematopoiesis. curr opin hematol. 2008 jan;15(1):49-58.
[4]. devi s, wang y, chew wk, lima r, a-gonzález n, mattar cn, chong sz, schlitzer a, bakocevic n, chew s, keeble jl, goh cc, li jl, evrard m, malleret b, larbi a, renia l, haniffa m, tan sm, chan jk, balabanian k, nagasawa t, bachelerie f, hidalgo a, ginhoux f, kubes p, ng lg. neutrophil mobilization via plerixafor-mediated cxcr4 inhibition arises from lung demargination and blockade of neutrophil homing to the bone marrow. j exp med. 2013 oct 21;210(11):2321-36.
[5]. mcdermott dh, liu q, velez d, lopez l, anaya-o'brien s, ulrick j, kwatemaa n, starling j, fleisher ta, priel da, merideth ma, giuntoli rl, evbuomwan mo, littel p, marquesen mm, hilligoss d, decastro r, grimes gj, hwang st, pittaluga s, calvo kr, stratton p, cowen ew, kuhns db, malech hl, murphy pm. a phase 1